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A 350619 hydrochloride

现货
Catalog No.
B5336
可溶性鸟苷酸环化酶(sGC)激活剂
组合的产品项目
规格价格库存 数量
10mg
¥ 4,016.00
Ship with 10-15 days

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Background

Km: 50 μM

Nitric oxide (NO) is a key mediator in many physiological processes and one of the key receptors through which NO exerts its effects is soluble guanylyl cyclase (GC). Guanylyl cyclase converts GTP to cyclic GMP that results in physiological processes such as smooth muscle relaxation, neurotransmission, platelet aggregation inhibition and immune response. A 350619 is a novel soluble guanylyl cyclase activator.

In vitro: A 350619 increased Vmax from 0.1 to 14.5 μmol/min/mg, and lowered Km from 300 to 50 μM. When A 350619 and YC-1 (another GC activator) were combined, a 156 fold increase in Vmax and a 5 fold decrease in Km were observed, indicating the modulation of the enzyme brought about by YC-1 and A 350619 are not additive, indicating a common binding site. Activation of soluble guanylyl cyclase by A 350619 was partially inhibited by ODQ, a specific inhibitor of soluble guanylyl cyclase by oxidation of the enzyme heme [1].

In vivo: Consistent with its biochemical activity, in a conscious rat model, A 350619 (1 μmol/kg) alone induced penile erection. Activation of soluble guanylyl cyclase in cavernosum tissue as an alternate method of enhancing the effect of NO may provide a novel treatment of sexual dysfunction [2].

Clinical trial: Up to now, A 350619 is still in the preclinical development stage.

Reference:
[1] Miller LN, Nakane M, Hsieh GC, Chang R, Kolasa T, Moreland RB, Brioni JD.  A 350619: a novel activator of soluble guanylyl cyclase. Life Sci. 2003 Jan 17;72(9):1015-25.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt425.41
Cas No.1217201-17-6
FormulaC21H25ClN2OS.HCl
Solubility≥21.25mg/mL in DMSO
Chemical Name(1Z,2E)-3-(2-((4-chlorophenyl)thio)phenyl)-N-(4-(dimethylamino)butyl)acrylimidic acid hydrochloride
SDFDownload SDF
Canonical SMILESCN(CCCC/N=C(O)/C([H])=C([H])/C1=CC=CC=C1SC2=CC=C(Cl)C=C2)C.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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化学结构

A 350619 hydrochloride