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製品番号: HY-14401

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Encaleret

(別名: CLTX-305; JTT-305; MK-5442)

カスタマーレビュー

Based on 1 Customer Validation

Encaleret (CLTX-305) is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC₅₀ of 12 nM. Encaleret exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.88%
CAS 番号: 787583-71-5
分子式: C₂₉H₃₃ClFNO₄
分子量:514.03

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Encaleret 構造式

CAS 番号: 787583-71-5

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- Cellular Effect
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Cellular Effect

Cell Line	Type	Value	Description	References
PC-12	IC₅₀	0.012 μM Compound: 15, JTT-305	Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay	[PMID: 24900301]

体内実験

Encaleret (1-3 mg/kg; oral administration; single dose) rapidly and transiently increases the level of endogenous parathyroid hormone in a dose-dependent manner in rats^[1].
Pharmacokinetic Analysis in Rats^[1]

Route	Dose (mg/kg)	T_max (h)	C_max (ng/mL)	T_1/2 (h)	BA (%)
p.o.	1	0.5	475	1.8	64

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 787583-71-5
性状 Solid
分子量 514.03
分子式 C₂₉H₃₃ClFNO₄
Color White to off-white
SMILES

O=C(C1=CC=C(C2=CC=CC=C2[C@H](OC[C@H](O)CNC(C)(C)CC3=CC=C(Cl)C(F)=C3)C)C=C1C)O
別名

CLTX-305; JTT-305; MK-5442
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 175 mg/mL (340.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9454 mL

9.7271 mL

19.4541 mL

5 mM

0.3891 mL

1.9454 mL

3.8908 mL

10 mM

0.1945 mL

0.9727 mL

1.9454 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Shinagawa Y, et al. Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone. ACS Med Chem Lett. 2010 Dec 29;2(3):238-42. [Content Brief]

[2]. Gafni RI, et al. Efficacy and Safety of Encaleret in Autosomal Dominant Hypocalcemia Type 1. N Engl J Med. 2023 Sep 28;389(13):1245-1247. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9454 mL	9.7271 mL	19.4541 mL	48.6353 mL
	5 mM	0.3891 mL	1.9454 mL	3.8908 mL	9.7271 mL
	10 mM	0.1945 mL	0.9727 mL	1.9454 mL	4.8635 mL
	15 mM	0.1297 mL	0.6485 mL	1.2969 mL	3.2424 mL
	20 mM	0.0973 mL	0.4864 mL	0.9727 mL	2.4318 mL
	25 mM	0.0778 mL	0.3891 mL	0.7782 mL	1.9454 mL
	30 mM	0.0648 mL	0.3242 mL	0.6485 mL	1.6212 mL
	40 mM	0.0486 mL	0.2432 mL	0.4864 mL	1.2159 mL
	50 mM	0.0389 mL	0.1945 mL	0.3891 mL	0.9727 mL
	60 mM	0.0324 mL	0.1621 mL	0.3242 mL	0.8106 mL
	80 mM	0.0243 mL	0.1216 mL	0.2432 mL	0.6079 mL
	100 mM	0.0195 mL	0.0973 mL	0.1945 mL	0.4864 mL

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

生物活性
- 製品説明
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外実験
純度とドキュメンテーション
参考文献

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Encaleret

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Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Encaleret

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Encaleret 関連分類

HY-14401 関連分類