DAPTA (acetate)
(Synonyms: D-Ala-peptide T-amide) 目录号 : GC48359
A CCR5 receptor antagonist
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
DAPTA is a peptide antagonist of chemokine (C-C motif) receptor 5 (CCR5).1 It inhibits CD4-dependent binding of HIV-1Ba-L and HIV-1CM235 gp120 envelope proteins to CCR5 (IC50s = 0.06 and 0.32 nM, respectively). DAPTA (0.1 mg/kg, i.p.) reduces marble burying and repetitive behavior, as well as decreases brain levels of IL-6, IL-9, and IL-17A, in the BTBR T+ Itpr3tf/J mouse model of autism spectrum disorder (ASD).2 It also reduces LPS-induced microglial activation and astrocyte hypertrophy in the dentate gyrus in a rat model of chronic neuroinflammation.3
1.Polianova, M.T., Ruscetti, F.W., Pert, C.B., et al.Chemokine receptor-5 (CCR5) is a receptor for the HIV entry inhibitor peptide T (DAPTA)Antiviral Res.67(2)83-92(2005) 2.Ahmad, S.F., Ansari, M.A., Nadeem, A., et al.DAPTA, a C-C chemokine receptor 5 (CCR5) antagonist attenuates immune aberrations by downregulating Th9/Th17 immune responses in BTBR T + Itpr3tf/J miceEur. J. Pharmacol.846100-108(2019) 3.Rosi, S., Pert, C.B., Ruff, M.R., et al.Chemokine receptor 5 antagonist D-Ala-peptide T-amide reduces microglia and astrocyte activation within the hippocampus in a neuroinflammatory rat model of Alzheimer's diseaseNeuroscience134(2)671-676(2005)
| Cas No. | SDF | ||
| 别名 | D-Ala-peptide T-amide | ||
| Canonical SMILES | OC(C=C1)=CC=C1C[C@@H](C(N[C@H](C(N)=O)[C@H](O)C)=O)NC([C@H](CC(N)=O)NC([C@H]([C@H](O)C)NC([C@H]([C@H](O)C)NC([C@H]([C@H](O)C)NC([C@H](CO)NC([C@H](N)C)=O)=O)=O)=O)=O)=O.CC(O)=O | ||
| 分子式 | C35H56N10O15•XC2H4O2 | 分子量 | 856.9 |
| 溶解度 | DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml | 储存条件 | -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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.167 mL | 5.835 mL | 11.67 mL |
| 5 mM | 0.2334 mL | 1.167 mL | 2.334 mL |
| 10 mM | 0.1167 mL | 0.5835 mL | 1.167 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。
acetate metabolism during hemodialysis
Artif Organs 1982 Nov;6(4):370-7.PMID:6762188DOI:10.1111/j.1525-1594.1982.tb04129.x.
We infused acetate into normal human subjects and performed kinetic analysis of the plasma and urine values obtained before, during, and after the infusion. The data were best fitted by a first-order elimination process with a mean metabolic clearance rate of 2.3 L/min. Gotch and Sargent had previously suggested that during dialysis, acetate metabolism was zero order. We performed kinetic modeling of acetate concentrations during dialysis. The data were best fitted to a Michaelis-Menton model (i.e., first-order metabolism at low concentrations and saturated at high concentrations). The mean Km for acetate in the dialysis patients was 8.5 mM and the mean Vmax was 18 mmol/min. Patients with a Vmax less than 7 mmol/min usually had a fall in plasma bicarbonate during dialysis while patients with a Vmax greater than 14 mmol/min usually had a rise in bicarbonate during dialysis. It is concluded that during high-surface-area dialysis, the capacity for acetate metabolism will affect acid-base homeostasis. Kinetic modeling will be useful to define acetate-intolerant patients and may be used to predict patients who will benefit from bicarbonate hemodialysis.
Acetate-buffered crystalloid fluids: Current knowledge, a systematic review
J Crit Care 2016 Oct;35:96-104.PMID:27481742DOI:10.1016/j.jcrc.2016.05.006.
Introduction: The concept of fluid resuscitation with balanced solutions containing acetate is relatively new. The knowledge about acetate mostly originates from nephrological research, as acetate was primarily used as a dialysis buffer where much higher doses of acetate are infused. The aim of this review is to give an overview of the advantages and disadvantages of an acetate-buffered crystalloid fluid when compared with other crystalloid infusates. Methods: We report trials with the primary object of comparing an acetate-buffered infusion solute to another crystalloid infusate. A systematic literature search of MEDLINE and the Cochrane Controlled Clinical trials register was conducted to identify suitable studies. Results: The search strategy used produced 1205 potential titles. After eliminating doubles, 312 titles and abstracts were screened, and 31 references were retrieved for full-text analysis. A total of 27 scientific studies were included in the study. Conclusion: Acetate-buffered crystalloid solutes do have a favorable influence on microcirculation. To what extent the acetate-buffered crystalloids influence kidney function is controversially discussed and not yet clear. Metabolic alkalosis did not occur in a single study in humans after an acetate-buffered infusate; potassium levels stayed stable in all studies. Cardiac output and contractility seem to be positively influenced; nonetheless, data on maintenance of a target blood pressure remain inconclusive. Whether acetate-buffered crystalloid fluids lead to lower rates of acute kidney injury and increased survival when compared with normal saline is yet unclear and may depend on the amount of fluid administered.
Acetate-mediated effects of ethanol
Alcohol Clin Exp Res 1994 Feb;18(1):144-8.PMID:8198211DOI:10.1111/j.1530-0277.1994.tb00894.x.
Ethanol has been shown to increase markedly portal blood flow, primarily by increasing intestinal blood flow. This effect of ethanol is reproduced by acetate, infused at rates equivalent to those leading to endogenous acetate production following ethanol administration. The physiological mediator, adenosine, is also known to increase markedly intestinal and portal tributary blood flow. We have shown that adenosine receptor blockade with 8-phenyltheophylline completely abolishes the effects of ethanol, acetate, and adenosine on intestinal and portal blood flow, suggesting that increases in adenosine tone may constitute a common mechanism mediating the actions of both ethanol and acetate on the splanchnic vasculature. Studies are also presented that show that acetate administration has marked effects on central nervous system function. On two tests, motor coordination and anesthetic potency, both ethanol and acetate showed similar effects. The effects of acetate were fully abolished by 8-phenyltheophylline. The effects of ethanol were partially blocked by 8-phenyltheophylline, with a greater effect of this blocker being seen at low doses of alcohol. Whereas ethanol at low doses increased locomotor activity in mice, acetate markedly reduced it. The effect of acetate on locomotion was fully reversed by the adenosine receptor blocker 8-phenyltheophylline, whereas the activating effect of ethanol on locomotion was markedly enhanced by this blocker. These data suggest that the actions of ethanol on locomotor activity normally result from the combination of a direct stimulatory effect of ethanol per se and an inhibitory effect of acetate, produced endogenously from ethanol. When the latter effect of acetate is abolished by adenosine receptor blockade, the activating effect of ethanol is fully expressed.(ABSTRACT TRUNCATED AT 250 WORDS)
Fragrance material review on phenethyl acetate
Food Chem Toxicol 2012 Sep;50 Suppl 2:S491-7.PMID:22414644DOI:10.1016/j.fct.2012.02.089.
A toxicologic and dermatologic review of phenethyl acetate when used as a fragrance ingredient is presented. Phenethyl acetate is a member of the fragrance structural group aryl alkyl alcohol simple acid esters (AAASAE). The AAASAE fragrance ingredients are prepared by reacting an aryl alkyl alcohol with a simple carboxylic acid (a chain of 1-4 carbons) to generate formate, acetate, propionate, butyrate, isobutyrate and carbonate esters. This review contains a detailed summary of all available toxicology and dermatology papers that are related to this individual fragrance ingredient and is not intended as a stand-alone document. Available data for phenethyl acetate were evaluated, then summarized, and includes: physical properties, acute toxicity, skin irritation, mucous membrane (eye) irritation, skin sensitization, elicitation, toxicokinetics, repeated dose, genotoxicity, and carcinogenicity data. A safety assessment of the entire AAASAE will be published simultaneously with this document. Please refer to Belsito et al. (2012) for an overall assessment of the safe use of this material and all AAASAE in fragrances.
Fragrance material review on anisyl acetate
Food Chem Toxicol 2012 Sep;50 Suppl 2:S467-70.PMID:22414654DOI:10.1016/j.fct.2012.02.083.
A toxicologic and dermatologic review of anisyl acetate when used as a fragrance ingredient is presented. Anisyl acetate is a member of the fragrance structural group Aryl Alkyl Alcohol Simple Acid Esters (AAASAE). The AAASAE fragrance ingredients are prepared by reacting an aryl alkyl alcohol with a simple carboxylic acid (a chain of 1-4 carbons) to generate formate, acetate, propionate, butyrate, isobutyrate and carbonate esters. This review contains a detailed summary of all available toxicology and dermatology papers that are related to this individual fragrance ingredient and is not intended as a stand-alone document. Available data for anisyl acetate were evaluated, then summarized, and includes: physical properties, skin irritation, skin sensitization, elicitation, and phototoxicity data. A safety assessment of the entire AAASAE will be published simultaneously with this document. Please refer to Belsito et al., 2012 for an overall assessment of the safe use of this material and all AAASAE in fragrances.