CH5447240
CH5447240 is an orally active agonist of parathyroid hormone receptor 1 (PTHR1). CH5447240 stimulates cAMP production in HKRK-B7 cells expressing hPTHR1, with an EC50 of 12 μM. CH5447240 exhibits PTH-like activity, elevating serum calcium and reducing serum phosphate. CH5447240 can be used for research on hypoparathyroidism.
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。
- CAS 番号: 1253919-92-4
- 分子式: C26H39N5O4S
- 分子量:517.68
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
PTH1R 12 μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| LLC-PK1 | EC50 |
12 μM
Compound: 1; CH5447240
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Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
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[PMID: 32022560] |
体外実験
CH5447240 (compound 1) stimulates cAMP production in HKRK-B7 cells expressing hPTHR1 with an EC50 of 12 μM and an EC20 of 3.0 μM; its NADPH-dependent clearance rate in human liver microsomes is 45 μL/min/mg[2].
CH5447240 can serve as a lead molecule for modification to obtain the derivative PCO371 (HY-100856)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Crl:CD(SD) (female, 6 weeks old)[2]
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Dosage:6, 19, or 60 mg/kg
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Administration:p.o.; once
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Result:Increased serum calcium and decreases serum phosphate in TPTX rats.
化学情報
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CAS 番号 1253919-92-4
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分子量 517.68
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分子式 C26H39N5O4S
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SMILES
O=C(N)N(C1=CC(C)=C(CCS(=O)(N(CC2)CCC2(NC([C@H]3CC[C@H](C)CC3)=N4)C4=O)=O)C(C)=C1)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Nishimura Y, et al. Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. Journal of medicinal chemistry. 2018 Jul 26;61(14):5949-5962. [Content Brief]
[2]. Nishimura Y, et al. Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist. Journal of medicinal chemistry. 2020 May 28;63(10):5089-5099. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CH5447240 関連分類
HY-120398 関連分類
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