PCA50941
目录号 : GC32568
PCA50941是1，4-二氢吡啶衍生物，可用于治疗心血管疾病。
Cas No.:136941-85-0
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
PCA50941 is a 1,4-dihydropyridine derivative, used for treatment for cardiovascular disease.
PCA50941 (1 μM) shifts the I-V relationship of whole-cell Ca2+ currents by about 5-10 mV towards more hyperpolarizing potentials. PCA50941 increases further the K(+)-evoked peak to 655 nM. In the presence of 5 mM Ca2+, PCA50941 increases the [Ca2+] peaks to 427 nM. PCA50941 potentiates the release of catecholamines from perfused bovine adrenal glands evoked by 30 s pulses of 17.7 mM K+ in a manner dependent on the [Ca2+]o[1].
PCA50941 (10-120 μM) by intracoronary injection, causes smaller reductions of coronary blood flow (CBF) in goats. PCA50941 (10-300 μM/min) does not modify CBF nor the other hemodynamic variables recorded by i.v. infusions in 4 goats. Intravenous infusion of PCA50941 (100 microg/min) reverses the hemodynamic variables from the shock state to control values within 20 min in 5 of 6 animals[2].
[1]. Montiel C, et al. Interactions between Ca2+, PCA50941 and Bay K 8644 in bovine chromaffin cells. Eur J Pharmacol. 1994 Aug 16;268(3):293-303. [2]. Fernández N, et al. PCA50941, a new 1,4-dihydropyridine, reverses endothelin-induced cardiogenic shock in the anesthetized goat. Life Sci. 1998;62(21):1933-42.
| Cas No. | 136941-85-0 | SDF | |
| Canonical SMILES | O=C(C1=C(C)NC(C)=C(C(OCC2CCCCO2)=O)C1C3=CC=CC([N+]([O-])=O)=C3)OCCN(C(C4=C5C=CC=C4)=O)S5(=O)=O | ||
| 分子式 | C30H31N3O10S | 分子量 | 625.65 |
| 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 | 1.5983 mL | 7.9917 mL | 15.9834 mL |
| 5 mM | 0.3197 mL | 1.5983 mL | 3.1967 mL |
| 10 mM | 0.1598 mL | 0.7992 mL | 1.5983 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。
PCA50941, a new 1,4-dihydropyridine, reverses endothelin-induced cardiogenic shock in the anesthetized goat
Life Sci 1998;62(21):1933-42.PMID:9619842DOI:10.1016/s0024-3205(98)00162-3.
This study was designed to test the hypothesis that the properties of novel 1,4-dihydropyridine PCA50941 could favor the recovery of cardiogenic shock. Coronary blood flow (CBF), measured with an electromagnetic flow probe placed on the left circumflex coronary artery, systemic arterial pressure and heart rate were recorded in 24 anesthetized goats; left ventricular pressure and dP/dt were also recorded in 19 of these goats. Under control conditions, intracoronary injections in 5 goats of PCA50941 (10-120 microg) caused smaller reductions of CBF than those of Bay K 8644 (0.3-10 microg) (the reduction of CBF by 120 microg PCA50941 was 25% and that by 10 microg Bay K 8644 was 43%), and i.v. infusions in 4 goats of PCA50941 (10-300 microg/min) did not modify CBF nor the other hemodynamic variables recorded, whereas i.v infusion of Bay K 8644 (10-30 microg/min) reduced CBF by 20% and increased arterial pressure, left ventricular pressure and dP/dt. During control conditions and endothelin-induced cardiogenic shock, respectively, the values for 15 goats were: for CBF, 33+/-4 vs. 16+/-4 ml/min; for mean arterial pressure, 88+/-4 vs. 60+/-5 mm Hg; for left ventricular systolic pressure, 102+/-5 vs. 75+/-4 mm Hg; for dP/dt, 1453+/-147 vs. 925+/-101 mm Hg/s (all P<0.05), and for heart rate, 77+/-6 vs. 81+/-6 beats/min (P>0.05). Intravenous infusion of PCA50941 (100 microg/min) reversed the hemodynamic variables from the shock state to control values within 20 min in 5 of 6 animals, whereas i.v. administration of Bay K 8644 (10-30 microg/min) was not effective in 4 of 5 animals, and the vehicle (DMSO) was not effective in none of 4 animals in reversing the hemodynamic shock state. Therefore, it is suggested that PCA50941, a novel 1,4-dihydropyridine, has a cardiovascular profile that might be suitable for treating cardiogenic shock states.
Interactions between Ca2+, PCA50941 and Bay K 8644 in bovine chromaffin cells
Eur J Pharmacol 1994 Aug 16;268(3):293-303.PMID:7528677DOI:10.1016/0922-4106(94)90053-1.
We describe here the effects of PCA50941 (a novel 1,4-dihydropyridine derivative) comparatively with Bay K 8644 on various parameters in bovine adrenal chromaffin cells. The binding of [3H](+)-isradipine to bovine adrenal medulla plasma membranes was inhibited similarly by PCA50941 and Bay K 8644 at various [Ca2+]o suggesting a common binding site for both compounds on the dihydropyridine receptor. In voltage-clamped chromaffin cells PCA50941 (1 microM) and Bay K 8644 (1 microM) shifted the I-V relationship of whole-cell Ca2+ currents by about 5-10 mV towards more hyperpolarizing potentials. At -20 mV, PCA50941 enhanced ICa by 195 +/- 16% and Bay K 8644 by 288 +/- 51%. Stimulation of fura 2-loaded chromaffin cell suspensions with 17.7 K+/0.5 Ca2+ increased 3-fold the basal [Ca2+]i. PCA50941 increased further the K(+)-evoked peak to 655 nM, and Bay K 8644 to 1129 nM. In the presence of 5 mM Ca2+, PCA50941 or Bay K 8644 increased the [Ca2+] peaks to 427 and 350 nM, respectively. PCA50941 potentiated the release of catecholamines from perfused bovine adrenal glands evoked by 30 s pulses of 17.7 mM K+ in a manner dependent on the [Ca2+]o. Thus at 1, 2.5, 5 and 10 mM Ca2+, secretion was 2.3-, 3.8-, 5- and 4-fold greater than in control glands. Bay K 8644 enhanced the K(+)-induced response 3- and 9-fold at [Ca2+]o of 0.25 or 0.5 mM, respectively; at higher [Ca2+]o the potentiation was similar to that of PCA50941.(ABSTRACT TRUNCATED AT 250 WORDS)