产品
编 号：F618341
分子式：C25H28Cl2N2O
分子量：443.41
分子式：C25H28Cl2N2O
分子量：443.41
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
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询价
25mg
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50mg
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结构图
CAS No: 2387505-78-2
产品详情
生物活性：
Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca2+-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM).
体内研究：
Calhex 231 (4.07 mg/kg（10 μmol/kg)；腹腔注射；每日一次；持续12周；雄性Wistar大鼠）治疗减轻了1型糖尿病模型 (T1D) 大鼠的糖尿病性心肌纤维化.Calhex-231 (Cal, 0.1-1 mg/kg) 通过改善血管低反应性和减少线粒体功能障碍，对创伤性出血性休克有缓解作用.Animal Model:Male Wistar rats (8 weeks old) injected with Streptozotocin
Dosage:4.07 mg/kg (10 μmol/kg)
Administration:Intraperitoneal injection; daily; for 12 weeks
Result:Ameliorated diabetic myocardial fibrosis in T1D rats.
Animal Model:Four hundred and fifty Sprague-Dawley (SD) rats (half male and half female).
Dosage:0.1, 1, or 5?mg/kg.
Administration:A continuous infusion.
Result:In all groups, MAP, LVSP, and ±dp/dtmax decreased significantly after shock. Administration of 5 or 1?mg/kg Cal resulted in significantly increased values at 1 and 2?hr postadministration, compared to rats in the LR only group (or 0.01). Rats treated with 1?mg/kg Cal demonstrated the greatest recovery. LR infusion induced short-term and slightly increase of blood pressor in normal rats.Cal (1?mg/kg) without LR infusion did not restore the decreased MAP after shock.
体外研究：
Calhex 231剂量依赖性地抑制了10 mM Ca2+ 诱导的IP反应，其在T764A (IC50 = 0.28 ± 0.05 μM) 和H766A (IC50 = 0.64 ± 0.03 μM) 突变受体中的效力与WT受体中的相似.Calhex 231治疗显著下调CaSR、α-SMA、Col-I/III、MMP2/9的表达。Calhex 231减轻了高糖诱导的心脏成纤维细胞中的心肌纤维化.Calhex 231能够抑制Itch（与阿特罗芬-1相互作用的蛋白4）-泛素蛋白酶体和TGF-β1/Smads途径，然后抑制心脏成纤维细胞的增殖，减少胶原沉积，缓解高糖诱导的心肌纤维化.
Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca2+-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM).
体内研究：
Calhex 231 (4.07 mg/kg（10 μmol/kg)；腹腔注射；每日一次；持续12周；雄性Wistar大鼠）治疗减轻了1型糖尿病模型 (T1D) 大鼠的糖尿病性心肌纤维化.Calhex-231 (Cal, 0.1-1 mg/kg) 通过改善血管低反应性和减少线粒体功能障碍，对创伤性出血性休克有缓解作用.Animal Model:Male Wistar rats (8 weeks old) injected with Streptozotocin
Dosage:4.07 mg/kg (10 μmol/kg)
Administration:Intraperitoneal injection; daily; for 12 weeks
Result:Ameliorated diabetic myocardial fibrosis in T1D rats.
Animal Model:Four hundred and fifty Sprague-Dawley (SD) rats (half male and half female).
Dosage:0.1, 1, or 5?mg/kg.
Administration:A continuous infusion.
Result:In all groups, MAP, LVSP, and ±dp/dtmax decreased significantly after shock. Administration of 5 or 1?mg/kg Cal resulted in significantly increased values at 1 and 2?hr postadministration, compared to rats in the LR only group (or 0.01). Rats treated with 1?mg/kg Cal demonstrated the greatest recovery. LR infusion induced short-term and slightly increase of blood pressor in normal rats.Cal (1?mg/kg) without LR infusion did not restore the decreased MAP after shock.
体外研究：
Calhex 231剂量依赖性地抑制了10 mM Ca2+ 诱导的IP反应，其在T764A (IC50 = 0.28 ± 0.05 μM) 和H766A (IC50 = 0.64 ± 0.03 μM) 突变受体中的效力与WT受体中的相似.Calhex 231治疗显著下调CaSR、α-SMA、Col-I/III、MMP2/9的表达。Calhex 231减轻了高糖诱导的心脏成纤维细胞中的心肌纤维化.Calhex 231能够抑制Itch（与阿特罗芬-1相互作用的蛋白4）-泛素蛋白酶体和TGF-β1/Smads途径，然后抑制心脏成纤维细胞的增殖，减少胶原沉积，缓解高糖诱导的心肌纤维化.
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