2. GPCR/G Protein
  3. CaSR
  4. Calhex 231

Calhex 231是一种强效的负向异构调节剂，能够阻断(IC50 = 0.39 μM)通过激活人类野生型 CaSR 瞬时钙感应受体引发的 [3H] 肌醇磷酸的增加。Calhex 231可用于创伤性出血性休克 (THS) 和糖尿病性心肌病 (DCM) 的研究.

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Calhex 231 Chemical Structure

Calhex 231 Chemical Structure

CAS No. : 652973-93-8

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Calhex 231 的其他形式现货产品:

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Calhex 231 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Calhex 231 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 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM)[1].

IC50 & Target

CaSR[1]
IC50: 0.39 μM (Inositol phosphate)[1]
体外研究
(In Vitro)

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[1].
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[2].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Calhex 231 相关抗体:

Cell Proliferation Assay[2]

Cell Line: Primary neonatal rat cardiac fibroblasts (CFs).
Concentration: 3 µM.
Incubation Time: 24 hours.
Result: Significantly decreased the proliferation of cardiac fibroblasts.
体内研究
(In Vivo)

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[2].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (8 weeks old) injected with Streptozotocin[2]
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)[3].
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.
分子量

406.95

Formula

C25H27ClN2O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Calhex 231 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Calhex 231652973-93-8Calhex231Calhex-231CaSRCalcium-sensing receptorDiabeticcardiomyopathyfibrosisG-proteinα-SMATGF-β1ItchcollagennegativeallostericinositolROSshock,Inhibitorinhibitorinhibit

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产品名称：
Calhex 231
目录号：
HY-103320
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