2. GPCR/G Protein
  3. CaSR
  4. Upacicalcet

Upacicalcet  (Synonyms: SK-1403 free acid; AJT240 free acid; PLS240 free acid)

目录号: HY-109106
产品使用指南 技术支持

Upacicalcet 是一种可作为 CaSR 激动剂 (EC50 = 10.8 nM) 的非肽拟钙剂。Upacicalcet 降低血清完整甲状旁腺激素 (iPTH) 和血清 Ca2+ 水平，降低低钙血症和胃肠道并发症。Upacicalcet 可改善 Adenine (HY-B0152) 诱导的继发性甲状旁腺功能亢进症 (SHPT) 大鼠模型的血管钙化和骨紊乱。Upacicalcet 抑制慢性肾脏病 (CKD) 大鼠皮质孔形成并减少骨纤维化。Upacicalcet 可用于研究 SHPT

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Upacicalcet sodium 通常具有更好的水溶性和稳定性。

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Upacicalcet

Upacicalcet Chemical Structure

CAS No. : 1333218-50-0

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Upacicalcet 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

Upacicalcet is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet is useful for studying SHPT[1][2].

IC50 & Target

calcium-sensing receptors[1]
体外研究
(In Vitro)

Upacicalcet (0.0001-10 μM) sodium 在 1.2mM Ca2+ 存在的情况下，在表达人类 CaSR 的 HEK293T (CaSR-HEK) 细胞中可增加细胞内 Ca2+ 和 IP-1 (EC50 = 26.1 nM)[1]。

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

Upacicalcet 相关抗体:
体内研究
(In Vivo)

Upacicalcet (0.3-30 mg/kg，静脉注射，一次) sodium 可降低雄性 SD 大鼠和双肾切除 SD 大鼠血清 iPTH、Ca2+ 和 Pi 水平，不影响雄性 SD 大鼠的胃排空[1]。
Upacicalcet (0.2-1 mg/kg，静脉注射，每周三次，三周) sodium 可降低 Adenine 诱导的 CKD SD 大鼠模型血清 iPTH 水平，并抑制甲状旁腺增生[2]。
Upacicalcet (1 mg/kg，皮下注射，每日一次，28 天) sodium 可降低 Adenine 诱导的 CKD Wistar 大鼠模型血清 iPTH 水平，并抑制异位钙化和皮质孔洞形成[2]。

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

Animal Model: Male SD rats[1]
Dosage: 0.03 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: i.v.; s.c., once
Result: Reduced serum iPTH, Ca2+, and Pi levels.
Did not affect gastric emptying.
Animal Model: Double-nephrectomized SD rats[1]
Dosage: 0.3 mg/kg, 3 mg/kg, 30 mg/kg
Administration: i.v., once
Result: Reduced serum iPTH, Ca2+ levels, lowered Ca2++ to a maximum of 8.2 mg/dL 24 hours after administration of 3 mg/kg or higher.
Animal Model: Adenine- induced (0.75 % Adenine in CE-2 solid diet) CKD Male SD rats (twelve-week-old) model[2]
Dosage: 0.2 mg/kg, 1 mg/kg
Administration: i.v., three times a week for 3 weeks
Result: Suppressed serum iPTH levels, increased phosphorus, creatinine and urea nitrogen levels.
Reduced parathyroid gland size by 44% and 57%, respectively, and decreased Ki-67 positive cell density compared to CKD controls.
Reduced Ca2+ content and von Kossa-positive area in the thoracic aorta.
Animal Model: Adenine-induced (0.75 % Adenine in CE-2 solid diet) renal failure male Wistar rats (nine-week-old) model[2]
Dosage: 1 mg/kg
Administration: s.c., once a day, 28 days
Result: Suppressed serum iPTH levels.
Inhibited the cortical porosity of the right femur and the volume of fibrosis in the right tibia.
分子量

351.76

Formula

C11H14ClN3O6S
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

Upacicalcet 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?

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Keywords:

Upacicalcet1333218-50-0SK-1403AJT240PLS240SK1403SK 1403AJT 240AJT-240PLS 240PLS-240CaSRCalcium-sensing receptorcalcium-sensing receptorscalcimimetic agentparathyroid hormonePTHsecondary hyperparathyroidismSHPTCaSR-HEK cellsCKDInhibitorinhibitorinhibit

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