货号:A464000 同义名: SB-262470A hydrochloride;NPS 2143 (hydrochloride)
NPS-2143 HCl (SB-262470A hydrochloride)是一种口服活性的钙感受器拮抗剂,选择性且高效地拮抗钙离子感受器(CaSR)。NPS-2143盐酸盐(SB-262470A盐酸盐)能够阻断在表达人体钙感受器的HEK 293细胞中通过激活钙离子受体引起的细胞内Ca2+浓度增加(IC50=43 nM)。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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免费溶解
产品名称 | CaSR ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
NPS-2143 |
++++
Ca(2+) receptor, IC50: 43 nM |
98+% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Calcium-sensing receptor (CaSR) is a G-protein coupled receptor expressed on the surface of parathyroid cells that mediates the secretion of parathyroid hormone (PTH). NPS-2143 hydrochloride is an antagonist for CaSR that inhibits the increase of cytoplasmic Ca2+ level induced by the activation of CaSR in HEK 293 cells expressing human CaSR with an IC50 value of 43 nM. NPS-2143 hydrochloride also stimulated the secretion of PTH from bovine parathyroid cells with an EC50 value of 41 nM[1]. In human astrocytes, incubation of NPS-2143 hydrochloride at 100 nM for 30 min inhibited the endogenous secretion of Aβ42/Aβ42-os. The treatment of NPS-2143 hydrochloride also promoted the translocation of hAPP to the plasma membrane in fAβ25-35± microglial cytokine mixture-exposed astrocytes[2]. Oral administration of NPS-2143 hydrochloride (100 μmol/kg) for 8 weeks led to a sustained elevation of plasma PTH level and a significant increase of bone turnover in osteopenic ovariectomized (OVX) rats. Daily oral administration of NPS-2143 hydrochloride (100 μmol/kg) for 5 weeks together with the treatment of 17β-estradiol increased cancellous bone area in OVX rats compared to their counterparts administered with 17β-estradiol alone[1]. |
作用机制 | NPS-2143 hydrochloride acts as an CaSR antagonist by binding to the cavity of the transmembrane domains of CaSR, thereby inhibiting its activation[3]. |
Dose | Mice: 45 mg/kg[4] (p.o.); 30 mg/kg[4] (i.p.) Rat: 1 mg/kg[5] (i.v.) |
Administration | p.o., i.p., i.v. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.25mL 0.45mL 0.22mL |
11.23mL 2.25mL 1.12mL |
22.45mL 4.49mL 2.25mL |
CAS号 | 324523-20-8 |
分子式 | C24H26Cl2N2O2 |
分子量 | 445.381 |
别名 | SB-262470A hydrochloride;NPS 2143 (hydrochloride);SB-262470A;NPS-2143 hydrochloride |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(235.75 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 1.5 mg/mL(3.37 mM),配合低频超声,并水浴加热至45℃助溶 |
动物实验配方 |