I-SAP
(Synonyms: Iodophenyl sulfonyl amino pinane Thromboxane A2, Iodophenyl sulfonyl amino pinane TXA2) 目录号 : GC43910A high-affinity TP receptor antagonist
Cas No.:133538-58-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
I-SAP is a high affinity TP receptor antagonist. At physiologic pH, I-SAP produces platelet shape change, but not aggregation, with an EC50 value of 9.7 nM. I-SAP binds to human platelets with the maximum binding obtained between pH 6.5 and pH 7.4. In washed human platelets, the Kd for I-SAP is 468 pM at pH 7.4 and 490 pM at pH 6.5.
Cas No. | 133538-58-6 | SDF | |
别名 | Iodophenyl sulfonyl amino pinane Thromboxane A2, Iodophenyl sulfonyl amino pinane TXA2 | ||
Canonical SMILES | CC1(C)[C@@H]2[C@H](C/C=C\CCCC(O)=O)[C@@H](N([H])S(C3=CC=C(I)C=C3)(=O)=O)C[C@H]1C2 | ||
分子式 | C22H30INO4S | 分子量 | 531.4 |
溶解度 | DMF: >50 mg/ml (from Pinane TXA2),DMSO: >25 mg/ml (from Pinane TXA2),Ethanol: >100 mg/ml (from Pinane TXA2),PBS pH 7.2: >100 µ g/ml (from Pinane TXA2) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.8818 mL | 9.4091 mL | 18.8182 mL |
5 mM | 0.3764 mL | 1.8818 mL | 3.7636 mL |
10 mM | 0.1882 mL | 0.9409 mL | 1.8818 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Nuclear imaging of amyloidosis
Pol J Radiol 2014 Jul 24;79:222-7.PMID:25071873DOI:10.12659/PJR.890147.
Summary Amyloidosis is a clinical condition caused by deposition of various protein fibrills in extracellular space. The presented symptoms depend on the type of deposits and the organ or organs involved. The correct diagnosis is often difficult, due to lack of nonivasive imaging techniques and insufficiency of morphological imaging procedures delievered by radiology. We presented a list of potential radiopharmaceuticals that can be used in detecting various types of amyloidoses. (123)I-SAP proved to have high sensitivity in imaging of AA and AL amyloidosis in visceral organs. (99m)Tc-Aprotinin was found to be useful in detecting cardiac amyloidosis. A couple of classical radiotracers, such as (201)Tl, (123)I-mIBG, together with (111)In-antimyosin were also tested for accuracy in cardiac imaging, however the main problem was low specificity. Potential applicability was also found in case of some bone-seeking agents and other radiotracers, e.g. (67)Ga-citrate and (99m)Tc-penta-DMSA. High sensitivity and specificity was achieved with β2-microglobulin labeled with (131)I or (111)In. Among PET tracers, (11)C-PIB deserves more attention, because it may have an important role in diagnosing of AD in the near future. Further clinical studies are expected to take place, because noninvasive diagnosing and monitoring of amyloidosis is still a challenge.
Delayed Absorption Superabsorbent Polymer for Strength Development in Concrete
Materials (Basel) 2022 Apr 7;15(8):2727.PMID:35454420DOI:10.3390/ma15082727.
Superabsorbent polymers (SAPs) are used as internal curing agents in cementitious materials, which reduce autogenous shrinkage in concrete as they have a low water-to-cement ratios and improve the freeze-thaw resistance. However, the compressive strength of concrete may also be reduced due to additional voids in the hydrated cement matrix. In this study, we fabricated a delayed absorption type of SAP (I-SAP) composed of cross-linked modified acrylate and studied its absorption characteristics and effect on compressive strength after 28 days. Furthermore, the effect of curing conditions on the strength of concrete and hydrated cement paste with SAP were investigated. The absorption capacity of I-SAP in the synthetic pore solution and deionised water was examined and compared with that of a conventional SAP, and the former was absorbed more by I-SAP. The results revealed that the compressive strength of concrete increased with the addition of I-SAP, particularly with the curing condition of 60% RH. Although the compressive strength of hydrated cement paste with I-SAP reduced in water or sealed curing conditions, no loss of strength in the paste cured at 60% RH was seen. The cement matrix densification due to hydration of belite around the SAP surface is the main mechanism for strength development in concrete cured at sealed and 60% RH. However, the voids formed by SAP control the compressive strength of hydrated paste.
Clinical characteristics and SAP scintigraphic findings in 10 patients with AGel amyloidosis
Amyloid 2014 Dec;21(4):276-81.PMID:25342098DOI:10.3109/13506129.2014.973105.
The clinical features of hereditary gelsolin (AGel) amyloidosis include corneal lattice dystrophy, distal sensorimotor, cranial neuropathy and cutis laxa. To date, four mutations of the gelsolin (GSN) gene encoding the following variants have been identified as the cause of this malady; p.D214N, p.D214Y, p.G194R and p.N211K (this nomenclature includes the 27-residue signal peptide). Interestingly, the latter two variants are associated exclusively with a renal amyloidosis phenotype. Here we report the clinical features in 10 patients with AGel amyloidosis associated with the p.D214N mutation, all of whom underwent whole body (123)I-SAP scintigraphy and were followed up in a single UK Centre for a prolonged period. Two patients, from the same kindred presented with proteinuria; eight subjects had a characteristic AGel amyloidosis phenotype including cranial neuropathy and/or corneal lattice dystrophy. (123)I-SAP scintigraphy revealed substantial renal amyloid deposits in all 10 patients, including those with preserved renal function, and usually without tracer uptake into other visceral organs. (123)I-SAP scintigraphy is a non-invasive technique that aids early diagnosis of patients with this rare disease, especially those who lack a family history and/or present with an unusual clinical phenotype.
Molecular imaging of amyloidosis: will the heart be the next target after the brain?
Curr Cardiol Rep 2012 Apr;14(2):226-33.PMID:22193845DOI:10.1007/s11886-011-0239-5.
Amyloidosis is a heterogeneous group of diseases with a common feature of extracellular deposition and infiltration of different types of amyloid fibrils in various organs. For example, Alzheimer's disease is characterized by deposition of amyloid β in the brain. Radiolabeled positron emission tomography (PET) tracers, mainly derivatives of thioflavin-T, were recently introduced for identification of amyloid β plaques in Alzheimer's patients. Such advances of amyloid β plaque imaging of the brain may shed light into imaging of other organs in amyloidosis patients, such as the heart. Cardiac infiltration of amyloid confers poor clinical outcomes, which renders early diagnosis for appropriate clinical management. At present, nuclear imaging of cardiac amyloidosis is predominantly accomplished with bone-seeking radiotracers, such as 99m-technetium-labeled pyrophosphate ((99m)Tc-PYP), 99m-technetium-methylene diphosphonate ((99m)Tc-MDP), and 99m-technetium-3,3,-diphosphono-1,2-propanodicarboxylic acid ((99m)Tc-DPD), with conflicting results in terms of diagnostic performance, with the exception for (99m)Tc-DPD, which may differentiate light-chain amyloidosis from transthyretin-related cardiac amyloidosis. Although other non-bone-seeking radiotracers such as iodine-123-labeled amyloid P component ((123)I-SAP), 123-iodine-Meta-iodobenzylguanidine ((123)I-mIBG), 99m-technetium-labeled protease inhibitor, and indium-111-labeled amyloid antibodies have also shown some success in identifying cardiac amyloidosis, the future, however, may lie in labeling derivatives of thioflavin-T. With the recent success of visualizing deposition of amyloid β in the brain, the US Food and Drug Administration-approved PET imaging agent (18)F-florbetapir may be used to target cardiac amyloidosis next.
¹⁸F-FDG PET/CT: a review of diagnostic and prognostic features in multiple myeloma and related disorders
Clin Exp Med 2015 Feb;15(1):1-18.PMID:25218739DOI:10.1007/s10238-014-0308-3.
Conventional radiographic skeletal survey has been for many years the gold standard to detect the occurrence of osteolytic lesions in patients with multiple myeloma (MM). However, the introduction of more sensitive imaging procedures has resulted in an updated anatomic and functional Durie and Salmon "plus" staging system and has remarkably changed the diagnostic and prognostic approach to this tumor. It is now established that (18)fluorine-fluorodeoxyglucose ((18)F-FDG) positron-emission tomography (PET) combined with low-dose computed tomography (CT), shortly designated PET/CT, exhibits a higher screening and diagnostic sensitivity and specificity over the skeleton X-ray. In patients with monoclonal gammopathy of undetermined significance and in those with smoldering MM, PET/CT is consistently unable to detect focal and/or diffuse marrow abnormalities. Conversely, based on a systematic review of 18 studies comprising almost 800 MM patients, PET/CT was able to detect MM osteolytic lesions with a sensitivity of approximately 80-90% and a specificity of 80-100%. Importantly, a poor degree of concordance has also been emphasized between PET/CT and whole-body magnetic resonance imaging (WB-MRI) in that when both techniques were applied to the same patients, double-positive results were recorded in approximately 30% of the cases, but in the majority of them, a higher number of lesions were revealed with PET/CT than with MRI. Double-negative results, on the other hand, were found in about 22% of the patients. Because PET/CT is able to identify tumor foci throughout the body, it can be usefully applied to the study of solitary bone plasmacytoma and extra-medullary plasmacytoma: In both conditions, the detection of additional, previously overlooked sites of skeletal involvement would falsify the diagnosis of single-district disease, upstage the tumor, and therefore require a different therapeutic approach. In addition, although PET/CT is poorly sensitive to diffuse bone marrow infiltration, it can anticipate a site of impending fracture throughout the body and can discriminate old from new pathologic fractures. MRI should, however, be preferred when vertebral bodies are suspected to be involved and the risk of vertebral fracture is to be assessed. PET/CT is a sensitive and reliable procedure to evaluate the response to chemotherapy and/or radiotherapy, which is shown by a remarkable reduction and sometimes total disappearance of FDG accumulation in the involved bony structures, although these structures remain morphologically abnormal. Conversely, an increased focal uptake of FDG in apparent remission patients often precedes clinically overt relapse. PET/CT should be preferred to other imaging techniques to assess the remission status after autologous stem cell transplantation. In patients with primary and remission-induced non-secretory MM, the use of PET/CT may help to early detect single or multiple districts of focal non-secretory relapse. Osteonecrosis of the jaw, its location, and extent in MM patients receiving bis-phosphonates are better defined by both PET/CT and contrast-enhanced MRI compared with dental panoramic views derived from cone beam CT imaging. Little is known as to the possible role of PET/CT in the assessment of disease extension, tumor load, and response to therapy in patients with Waldenström's macroglobulinemia (WM). In a study conducted on 35 WM patients, comparative PET/CT before and after therapy was able to detect positive findings in 83% of the patients, in contrast with the previous results achieved with conventional imaging that reported visceral involvement in much lower percentages. Similarly scanty are the data on the use of PET/CT in localized and systemic amyloidosis, given the small number of patients studied so far. A retrospective study has shown that, at variance from (123)Iodine-serum amyloid P component ((123)I-SAP) scintigraphy, which was found to be positive in about one-third of the patients with localized amyloidosis, an increased FDG uptake was detected at the amyloid site in virtually all of them. On the contrary, none of the patients with systemic amyloidosis showed an increased FDG uptake in sites of known deposition, whereas (123)I-SAP scintigraphy tested positive in the large majority of them. In another study, however, no such remarkable difference of positive PET/CT scans between localized and systemic amyloidosis was reported. Finally, false-positive and false-negative PET/CT findings can occur in different conditions that should be kept in mind to avoid wrong or omitted diagnoses.