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AS-35 Sale

目录号 : GC31774

AS-35是一种有效的,可口服的,选择性的leukotrienes拮抗剂,抑制LTC4,LTD4和LTE4诱导的回肠收缩,IC50值分别为8nM,4nM和3nM,具有抗过敏的功效。

AS-35 Chemical Structure

Cas No.:108427-72-1

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产品描述

AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.

In isolated guinea pig preparations, AS-35 antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively. In the trachea, the agent also antagonizes LTD4 and LTE4-induced con tractions with IC50 values of 10 nM and 20 nM, respectively. However, AS-35 does not antagonize LTC4-induced tracheal contraction in the presence of L-serine borate[1].

AS-35 (0.0375 to 0.3 mg/kg, i.v.) dose-dependently antagonizes bronchoconstriction induced by i.v.-injection of LTC4 and LTD4 in anesthetized guinea pigs, but does not inhibit histamine-induced bronchoconstriction. Oral administration of AS-35 also antagonizes LTD4 as well as antigen-induced LT-mediated bronchoconstriction. AS-35 (p.o.) inhibits LTD4-induced increase in the cutaneous vascular permeability of guinea pig[1].

[1]. Kasai H, et al. Peptide leukotriene antagonistic activity of AS-35, a new antiallergic drug. Jpn J Pharmacol. 1992 Apr;58(4):347-55.

Chemical Properties

Cas No. 108427-72-1 SDF
Canonical SMILES O=C1C(C2=NN=NN2)=CN=C3N1C=CC=C3COC4=CC=C(C(C)=O)C(O)=C4CCC
分子式 C21H20N6O4 分子量 420.42
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 2.3786 mL 11.8929 mL 23.7857 mL
5 mM 0.4757 mL 2.3786 mL 4.7571 mL
10 mM 0.2379 mL 1.1893 mL 2.3786 mL
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Research Update

Global burden of preterm birth

Preterm birth is a live birth that occurs before 37 completed weeks of pregnancy. Approximately 15 million babies are born preterm annually worldwide, indicating a global preterm birth rate of about 11%. With 1 million children dying due to preterm birth before the age of 5 years, preterm birth is the leading cause of death among children, accounting for 18% of all deaths among children aged under 5 years and as much as 35% of all deaths among newborns (aged <28 days). There are significant variations in preterm birth rates and mortality between countries and within countries. However, the burden of preterm birth is particularly high in low- and middle-income countries, especially those in Southeast Asia and sub-Saharan Africa. Preterm birth rates are rising in many countries. The issue of preterm birth is of paramount significance for achieving United Nations Sustainable Development Goal 3 target #3.2, which aims to end all preventable deaths of newborns and children aged under 5 years by 2030.

Recombineering: genetic engineering in bacteria using homologous recombination

The bacterial chromosome and bacterial plasmids can be engineered in vivo by homologous recombination using PCR products and synthetic oligonucleotides as substrates. This is possible because bacteriophage-encoded recombination proteins efficiently recombine sequences with homologies as short as 35 to 50 bases. Recombineering allows DNA sequences to be inserted or deleted without regard to location of restriction sites. This unit first describes preparation of electrocompetent cells expressing the recombineering functions and their transformation with dsDNA or ssDNA. It then presents support protocols that describe several two-step selection/counter-selection methods of making genetic alterations without leaving any unwanted changes in the targeted DNA, and a method for retrieving onto a plasmid a genetic marker (cloning by retrieval) from the Escherichia coli chromosome or a co-electroporated DNA fragment. Additional protocols describe methods to screen for unselected mutations, removal of the defective prophage from recombineering strains, and other useful techniques.

[Oocyt donation]

The number of treatments with donated oocytes has risen markedly in Denmark during the latest decade due to changes in legislation and because female age is increasingly advanced when fertility treatment is warranted. Today, oocyte donation is a standard procedure offering the otherwise untreatable a high chance of achieving a pregnancy. Live birth rates as high as 35% per treatment are being reported. It is, however, important to be aware of increased risks of hypertensive disorders and bleeding complications in these pregnancies. As pointed out in this review, continuous research in the field is therefore highly needed.

Junctional Ectopic Tachycardia

Junctional ectopic tachycardia (JET) is an arrhythmia present usually in infants and children. It originates in the atrioventricular (AV) node or AV junction, including the bundle of His (BH). It is further classified into congenital junctional ectopic tachycardia (CJET) and postoperative junctional ectopic tachycardia (POJET).

CJET occurs without any previous history of heart surgery and can be even present at birth. CJET is associated with high morbidity and mortality as high as 35 percent if not diagnosed and appropriately treated as it is usually refractory to medical therapy.

POJET usually occurs in the first 72 hours of repair of congenital heart defects. It has been attributed to ischemia, stretching, and direct injury to the atrioventricular (AV) conduction tissue of the heart during the repair of congenital defects. It can be regular or irregular. It does not involve the reentry circuit, unlike AV nodal reentry and AV reentry supraventricular arrhythmias. It could have retrograde atrial conduction in 1:1 pattern or AV dissociation with variable conduction.

Atmospheric washout of 35S during single rain events - Implications for 35S sampling schemes

Cosmogenic radiosulfur (35S; half-life: 87.4 days) is transferred with the rain to the groundwater (as 35SO42-) and can be used as residence time tracer for the detection of sub-yearly groundwater residence times. Due to the distinct but non-regular annual 35S pattern in precipitation, related data evaluation requires consideration of a35S input function that is based on representative rain samples. While minor rain events can easily be sampled quantitatively and hence representatively, a long-lasting rain event may get documented by a sample that represents only a certain sequence of the event, thus potentially resulting in a35S activity concentration that might not be representative. With the aim to examine the magnitude of temporal variations of the 35S activity concentration in rain during long-lasting rain events, we present and discuss two related exemplary 35S time series. Furthermore, we evaluate the applicability of the parameters total sulfate and electrical conductivity (EC), both detected in rainwater as easily attainable 35S proxies. The results of the study show (i) that the 35S activity concentration may vary substantially during long-lasting rain events due to atmospheric migration processes and aerosol washout and (ii) that neither sulfate nor EC are suitable as 35S proxies due to the different origin of 35S on the one hand and sulfate/EC on the other. Hence, for the determination of a35S activity concentration that is representative for a long-lasting rain event 35S analyses of an adequate number of sub-samples cannot be avoided.