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.
For research use only. We do not sell to patients.
- CAS No.: 1253919-92-4
- Formula: C26H39N5O4S
- Molecular Weight:517.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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] |
In Vitro
CH5447240 (12 μM; preincubation for 5 min; reaction at 37 °C for 30 min) forms a GSH adduct in human liver microsomes, indicating the generation of a reactive metabolite[2].
CH5447240 (compound 14I) binds to human PTHR1 in COS-7 cell membranes in radioligand competition assays with an IC50 of 93.7 μM; it exhibits low hERG channel inhibition, producing 10% inhibition at 10 μM[1].
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
In Vivo
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.
Chemical Information
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CAS No. 1253919-92-4
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Molecular Weight 517.68
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CH5447240 Related Classifications
HY-120398 Related Classifications
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