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Cat. No.: HY-186200

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PTHR1 antagonist 1

PTHR1 antagonist 1 is a PTHR1 antagonist with an IC₅₀ of 0.090 µM. PTHR1 antagonist 1 is applicable to the research of calcium metabolism disorders.

For research use only. We do not sell to patients.

CAS No.: 2458230-46-9
Formula: C₂₉H₃₀ClN₅O₂
Molecular Weight:516.03

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PTHR1 antagonist 1 Chemical Structure

CAS No.: 2458230-46-9

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
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Biological Activity

Description

PTHR1 antagonist 1 is a PTHR1 antagonist with an IC₅₀ of 0.090 µM. PTHR1 antagonist 1 is applicable to the research of calcium metabolism disorders^[1].

IC₅₀ & Target^[1]

PTH1R

0.090 μM (IC₅₀)

All PTHR Isoforms :

PTH1R
PTH2R

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	0.09 μM Compound: 18	Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins	[PMID: 32345459]

In Vitro

PTHR1 antagonist 1 (Compound 18) (10-100 µM; 30 min) potently inhibits PTHR1-induced cAMP production in CHO-K1 cells expressing PTHR1, with an IC₅₀ of 0.090 µM^[1].
After incubation with rat liver microsomes for 0.5 h, 34% of PTHR1 antagonist 1 (1 µM; 20 min) remains, indicating that it has moderate metabolic stability in this system^[1].

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

Chemical Information

CAS No. 2458230-46-9
Molecular Weight 516.03
Formula C₂₉H₃₀ClN₅O₂
SMILES

N#CC1=CC2=C(C3=CC(Cl)=CN=C3C(C)(C)C(N2C4=CC=C(NCCNC5CCOCC5)C=C4)=O)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Arai Y, et al. Discovery of novel, potent, and orally bioavailable pyrido[2,3-d][1]benzazepin-6-one antagonists for parathyroid hormone receptor 1. Bioorg Med Chem. 2020;28(11):115524. [Content Brief]

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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.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PTHR1 antagonist 1

All PTHR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PTHR1 antagonist 1 Related Classifications

HY-186200 Related Classifications