Tecalcet Hydrochloride R-568 hydrochloride|cas:177172-49-5|西域试剂

Tecalcet Hydrochloride R-568 hydrochloride,99.74%

产品编号：Bellancom-10167A| CAS NO：177172-49-5| 分子式：C₁₈H₂₃Cl₂NO| 分子量：340.29

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货号	价格	库存与货期
Bellancom-10167A	￥1450.00	杭州北京（现货）
Bellancom-10167A	￥2380.00	杭州北京（现货）
Bellancom-10167A	￥5250.00	杭州北京（现货）
Bellancom-10167A	￥8650.00	杭州北京（现货）

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Tecalcet Hydrochloride R-568 hydrochloride

产品介绍

Tecalcet Hydrochloride (R 568 Hydrochloride) 是一个口服有效的拟钙剂，变构正调控钙敏感受体 (CaSR)。Tecalcet Hydrochloride (R 568 Hydrochloride) 可提高激活细胞外Ca²⁺的敏感性。

生物活性

Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca²⁺.

体外研究

Tecalcet (NPS 568, 0.1-100 μM) increase [Ca²⁺]i in a concentrationdependent and stereoselective manner.
Tecalcet (NPS 568, 0.1-100 nM) shiftes the concentration-response curve for extracellular Ca²⁺ to the left without affecting the maximal response and, thereby, decreases the EC₅₀ value for extracellular Ca21 to 0.61±0.04 mM.

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

体内研究

Tecalcet (1.5 and 15 mg/kg, orally, twice daily for 4 days) inhibits PT cell proliferation in rats with renal insufficiency.

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

Animal Model:	10-wk-old Male Sprague-Dawley rats weighing 310-350 g.
Dosage:	1.5 and 15 mg/kg.
Administration:	Orally twice daily for 4 days.
Result:	Did not significantly change serum 1,25 (OH)₂D₃ levels. In contrast, serum PTH levels were reduced by in a dose-dependent manner. Clearly reduced the number of BrdU-positive PT cells by 20% at a low dose (1.5 mg/kg body wt), and by 50% at a high dose (15 mg/kg body wt), indicating an antiproliferative effect on PT cells. Reduced PT cell volume in a dose-dependent manner.

体内研究

Tecalcet (1.5 and 15 mg/kg, orally, twice daily for 4 days) inhibits PT cell proliferation in rats with renal insufficiency.

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

Animal Model:	10-wk-old Male Sprague-Dawley rats weighing 310-350 g.
Dosage:	1.5 and 15 mg/kg.
Administration:	Orally twice daily for 4 days.
Result:	Did not significantly change serum 1,25 (OH)₂D₃ levels. In contrast, serum PTH levels were reduced by in a dose-dependent manner. Clearly reduced the number of BrdU-positive PT cells by 20% at a low dose (1.5 mg/kg body wt), and by 50% at a high dose (15 mg/kg body wt), indicating an antiproliferative effect on PT cells. Reduced PT cell volume in a dose-dependent manner.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (146.93 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9387 mL	14.6933 mL	29.3867 mL
5 mM	0.5877 mL	2.9387 mL	5.8773 mL
10 mM	0.2939 mL	1.4693 mL	2.9387 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: 2.5 mg/mL (7.35 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.35 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。