Calhex 231 hydrochloride 是一种通过负变构调节来抑制CaSR的。Calhex 231 hydrochloride 在 HEK293 细胞中阻断 Ca2+诱导的肌醇磷酸酯的积累，IC50为 0.39 μM。Calhex 231 hydrochloride 可用于糖尿病性心肌病 (DCM) 的研究。
| 生物活性 | Calhex 231 hydrochloride is aCaSRinhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca2+-induced accumulation of [3H]inositol phosphate with anIC50of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment[1][2]. |
| IC50& Target | CaSR[1]
IC50: 0.39 μM (Inositol phosphate)[2] |
体外研究
(In Vitro) | Calhex 231 treatment significantly decreases the proliferation of cardiac fibroblasts[1].
Calhex 231 treatment significantly downregulates the CaSR, α-SMA, Col-I/III, MMP2/9 expresses. Calhex231 alleviates high glucose-induced myocardial fibrosis in cardiac fibroblasts[1].
Calhex 231 could inhibit Itch (atrophin-1 interacting protein 4)-ubiquitin proteasome and TGF-β1/Smads pathways, and then depress the proliferation of cardiac fibroblasts, along with the reduction deposition of collagen, alleviate glucose-induced myocardial fibrosis[1].
Cell Proliferation Assay[1] | Cell Line: | Primary neonatal rat cardiac fibroblasts (CFs) | | Concentration: | 3 μM | | Incubation Time: | 24 hours | | Result: | Significantly decreased the proliferation of cardiac fibroblasts. |
Western Blot Analysis[1] | Cell Line: | Primary neonatal rat cardiac fibroblasts (CFs) | | Concentration: | 3 μM | | Incubation Time: | 48 hours | | Result: | The expression of CaSR, α-SMA, Col-I/III, MMP2/9 were significantly downregulated. |
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体内研究
(In Vivo) | Calhex 231 (4.07 mg/kg (10 μmol/kg); intraperitoneal injection; daily; for 12 weeks; male Wistar rats) treatment ameliorates diabetic myocardial fibrosis in type 1 diabetic model (T1D) rats[1].
| Animal Model: | Male Wistar rats (8 weeks old) injected with Streptozotocin[1] | | Dosage: | 4.07 mg/kg (10 μmol/kg) | | Administration: | Intraperitoneal injection; daily; for 12 weeks | | Result: | Ameliorated diabetic myocardial fibrosis in T1D rats. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(75.17 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2552 mL | 11.2762 mL | 22.5525 mL | | 5 mM | 0.4510 mL | 2.2552 mL | 4.5105 mL | | 10 mM | 0.2255 mL | 1.1276 mL | 2.2552 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (5.64 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (5.64 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.64 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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