Sch-42495 racemate
目录号 : GC31318
Sch-42495racemate是Sch-42495的外消旋体。Sch-42495是一种新型的中性金属内肽酶(NEP)抑制剂。Sch-42495是SCH42354的口服活性前药。
Cas No.:145841-10-7
Sample solution is provided at 25 µL, 10mM.
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Sch-42495 racemate is the racemate of Sch-42495. Sch-42495 is a novel neutral metalloendopeptidase (NEP) inhibitor. Sch-42495 is the orally active ethylester prodrug of SCH 42354.
SCH 42354 selectively inhibits hydrolysis of leu-enkephalin and ANF (IC50 of 8.3 and 10.0 nM, respectively) in vitro[1].
Plasma levels of exogenous atrial natriuretic factor (ANF) are augmented and ANF clearance from plasma is delayed by oral Sch-42495 (3 to 30 mg/kg) in normotensive rats. Plasma ANF levels in volume expanded rats are higher in Sch-42495-treated rats. Diuretic and natriuretic effects of ANF are increased in rats treated with Sch-42495. In Dahl-S hypertensive rats, Sch-42495 (1 to 10 mg/kg orally) produces falls in blood pressure of a magnitude similar to that observed in DOCA-Na hypertensive rats. Significant hypotensive activity is observed 18 h after a single 10 mg/kg oral dose in Dahl-S hypertensive rats. In DOCA-Na hypertensive rats, a single dose of Sch-42495 significantly decreases cardiac output and does not lower systemic vascular resistance, a profile similar to that of ANF[1]. Spontaneously hypertensive rats (SHR) aged 9 to 10 weeks are injected with either Streptozotocin (45 mg/kg) or citrate buffer and randomized to receive either Captopril (25 mg/kg BID), Sch-42495 (30 mg/kg BID), S21402 (25 or 50 mg/kg BID), or vehicle by gavage for 4 weeks. A group of diabetic SHR is also allocated to receive the combination of Sch-42495 (30 mg/kg BID) and Captopril (25 mg/kg BID). The degree of renal NEP inhibition is determined by autoradiography, and plasma renin activity (PRA) is determined by radioimmunoassay. In nondiabetic SHR, S21402 and Captopril are equally effective. Relative heart weight decreases in parallel to the changes in blood pressure. Renal NEP is clearly inhibited (70% to 92%; P
[1]. Watkins RW, et al. Atrial natriuretic factor potentiating and hemodynamic effects of SCH 42495, a new, neutral metalloendopeptidase inhibitor. Am J Hypertens. 1993 May;6(5 Pt 1):357-68. [2]. Tikkanen T, et al. Dual inhibition of neutral endopeptidase and angiotensin-converting enzyme in rats with hypertension and diabetes mellitus. Hypertension. 1998 Oct;32(4):778-85.
Animal experiment: | Rats[2] Streptozotocin-injected and citrate buffer–injected SHR are randomly allocated to receive by gavage Captopril Captopril (25 mg/kg BID in distilled water), Sch-42495 (30 mg/kg BID in 5% arabic gum), S21402 at 2 different doses (25 mg/kg BID or 50 mg/kg BID in 5% arabic gum), or vehicle for 4 weeks starting on the day of Streptozotocin or buffer injection. The choice of the 2 doses of S21402 is based on previous findings suggesting that sufficient renal NEP inhibition, comparable to 30 mg/kg of Sch-42495, may be obtained with 25 mg/kg of S21402, while 50 mg/kg of S21402 is needed to provide equipotent angiotensin I pressor response inhibitory efficacy compared with 25 mg/kg of Captopril. A group of diabetic SHR is also allocated to receive the combination of Sch-42495 (30 mg/kg BID) and Captopril (25 mg/kg BID) by gavage. |
References: [1]. Watkins RW, et al. Atrial natriuretic factor potentiating and hemodynamic effects of SCH 42495, a new, neutral metalloendopeptidase inhibitor. Am J Hypertens. 1993 May;6(5 Pt 1):357-68. | |
| Cas No. | 145841-10-7 | SDF | |
| Canonical SMILES | CSCC[C@@H](C(OCC)=O)NC(C(CSC(C)=O)CC1=CC=CC=C1C)=O | ||
| 分子式 | C20H29NO4S2 | 分子量 | 411.58 |
| 溶解度 | Soluble 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 | 2.4297 mL | 12.1483 mL | 24.2966 mL |
| 5 mM | 0.4859 mL | 2.4297 mL | 4.8593 mL |
| 10 mM | 0.243 mL | 1.2148 mL | 2.4297 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。
Quality Control & SDS
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- Purity: >98.00%
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