A 350619 hydrochloride
目录号 : GC13555
Activator of soluble guanylyl cyclase (sGC)
Cas No.:1217201-17-6
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
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.
| Cas No. | 1217201-17-6 | SDF | |
| 化学名 | (1Z,2E)-3-(2-((4-chlorophenyl)thio)phenyl)-N-(4-(dimethylamino)butyl)acrylimidic acid hydrochloride | ||
| Canonical SMILES | CN(CCCC/N=C(O)/C([H])=C([H])/C1=CC=CC=C1SC2=CC=C(Cl)C=C2)C.Cl | ||
| 分子式 | C21H25ClN2OS.HCl | 分子量 | 425.41 |
| 溶解度 | ≥ 21.25mg/mL in DMSO | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3507 mL | 11.7534 mL | 23.5067 mL |
| 5 mM | 0.4701 mL | 2.3507 mL | 4.7013 mL |
| 10 mM | 0.2351 mL | 1.1753 mL | 2.3507 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。