Calcium-sensing R/CaSR 蛋白, Human (HEK293, His)

Calcium-sensing receptor (CaSR) is a G-protein-coupled receptor that is essential for maintaining calcium homeostasis. It senses changes in extracellular calcium concentration, regulates parathyroid hormone (PTH) production, and activates the phosphatidylinositol-calcium second messenger system. Calcium-sensing R/CaSR Protein, Human (HEK293, His) is the recombinant human-derived Calcium-sensing R/CaSR protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Calcium-sensing R/CaSR Protein, Human (HEK293, His) is 582 a.a., with molecular weight of approximately 95-130 kDa.

钙敏感 R/CaSR 蛋白是一种 G 蛋白偶联受体，在检测细胞外钙浓度变化方面发挥着关键作用，这对于维持钙稳态至关重要。该受体感知循环钙水平的波动并调节甲状旁腺中甲状旁腺激素（PTH）的产生。其活性由激活磷脂酰肌醇-钙第二信使系统的 G 蛋白介导。受体的激活涉及共激动剂机制，其中色氨酸或苯丙氨酸等芳香族氨基酸与钙或镁等二价阳离子协同作用，实现完全激活。在静息状态下，受体采用开放构象，阴离子结合促进非活性构象。芳香族氨基酸结合后，细胞外捕蝇草模块凹槽关闭，在亚基之间诱导新的同二聚体界面。钙离子通过增强膜近端结构域之间的同二聚体相互作用进一步稳定活性状态。值得注意的是，该受体可以被 AMG 416 激活，AMG 416 是一种含 D-氨基酸的肽激动剂，正在评估用于治疗接受血液透析的慢性肾病患者的继发性甲状旁腺功能亢进症，AMG 416 通过与 Cys-482 形成二硫键发挥作用。

Measured by its ability to inhibit the proliferation of HT-29 cells. The ED₅₀ for this effect is 38.93 ng/mL, corresponding to a specific activity is 25687.131 U/mg.

• 
  Measured by its ability to inhibit the proliferation of HT-29 cells. The ED₅₀ for this effect is 38.93 ng/mL, corresponding to a specific activity is 25687.131 U/mg.

Human

HEK293

C-6*His

P41180-1 (Y20-K601)

846  [NCBI]

YGPDQRAQKKGDIILGGLFPIHFGVAAKDQDLKSRPESVECIRYNFRGFRWLQAMIFAIEEINSSPALLPNLTLGYRIFDTCNTVSKALEATLSFVAQNKIDSLNLDEFCNCSEHIPSTIAVVGATGSGVSTAVANLLGLFYIPQVSYASSSRLLSNKNQFKSFLRTIPNDEHQATAMADIIEYFRWNWVGTIAADDDYGRPGIEKFREEAEERDICIDFSELISQYSDEEEIQHVVEVIQNSTAKVIVVFSSGPDLEPLIKEIVRRNITGKIWLASEAWASSSLIAMPQYFHVVGGTIGFALKAGQIPGFREFLKKVHPRKSVHNGFAKEFWEETFNCHLQEGAKGPLPVDTFLRGHEESGDRFSNSSTAFRPLCTGDENISSVETPYIDYTHLRISYNVYLAVYSIAHALQDIYTCLPGRGLFTNGSCADIKKVEAWQVLKHLRHLNFTNNMGEQVTFDECGDLVGNYSIINWHLSPEDGSIVFKEVGYYNVYAKKGERLFINEEKILWSGFSREVPFSNCSRDCLAGTRKGIIEGEPTCCFECVECPDGEYSDETDASACNKCPDDFWSNENHTSCIAK

approximately 95-130 kDa

• 
  Greater than 95% as determined by reducing SDS-PAGE.

无菌粉末.

Lyophilized from a 0.2 μm filtered solution of PBS, pH 7.4.

<1 EU/μg, determined by LAL method.

It is not recommended to reconstitute to a concentration less than 100 μg/mL in ddH₂O. For long term storage it is recommended to add a carrier protein (0.1% BSA, 5% HSA, 10% FBS or 5% Trehalose).

Stored at -20°C for 2 years. After reconstitution, it is stable at 4°C for 1 week or -20°C for longer (with carrier protein). It is recommended to freeze aliquots at -20°C or -80°C for extended storage.

Room temperature in continental US; may vary elsewhere.