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Cat. No.: HY-131206

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DS37571084

DS37571084 is an orally active competitive antagonist of parathyroid hormone receptor 1 (PTH1R) with an IC₅₀ value of 0.17 μM. DS37571084 is applicable to the research of bone diseases and calcium metabolism disorders associated with primary hyperparathyroidism.

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

CAS No.: 2460353-87-9
Formula: C₂₈H₃₀Cl₂N₄O₂
Molecular Weight:525.47

Storage:

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

Data Sheet (283 KB)

DS37571084 Chemical Structure

CAS No.: 2460353-87-9

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[2]

PTH1R

0.17 μM (IC₅₀)

All PTHR Isoforms :

PTH1R
PTH2R

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC50	0.17 μM	Inhibition of PTH-induced cAMP production in cAMP Hunter™ CHO-K1 PTHR1 Gs/Gq cells incubated for 30 min using a cAMP dynamic 2 kit. Inhibition of PTH-induced cAMP production in cAMP Hunter™ CHO-K1 PTHR1 Gs/Gq cells incubated for 30 min using a cAMP dynamic 2 kit.	39519190

In Vitro

DS37571084 (10-100 μM; 30 min) potently inhibits PTHR1-induced cAMP production in cAMP Hunter™ CHO-K1 PTHR1 Gs/Gq cells with an IC₅₀ of 0.17 μM^[1].
DS37571084 exhibits metabolic stability in rat liver microsomes, with 65% of the compound remaining after 20 min of incubation at 1 μM^[1].
DS37571084 shows no significant inhibitory activity against CYP 1A2, CYP 2C8, CYP 2C9, CYP 2C19, CYP 2D6, or CYP 3A4 at a concentration of 10 μM^[1].

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

Parmacokinetics

Species	Dose	Route	Bioavailability	AUC_last	T_1/2	CL	V_d
Rat^[1]	10 mg/kg	p.o.	61 %	2.50 μg·h/mL	13.1 h	/	/
Rat^[1]	5 mg/kg	i.v.	/	/	/	39.0 mL/min/kg	29.4 L/kg

Chemical Information

CAS No. 2460353-87-9
Molecular Weight 525.47
Formula C₂₈H₃₀Cl₂N₄O₂
SMILES

O=C1N(C2=CC=C(NCCNC3CCOCC3)C=C2)C4=CC(Cl)=CC=C4C5=CC(Cl)=CN=C5C1(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
COA (2659 KB)
Elemental Analysis Report (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)
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. Bioorganic & medicinal chemistry. 2020 Jun 01;28(11):115524. [Content Brief]

[2]. Iwanowska M, et al. Bone Disease in Primary Hyperparathyroidism-Changes Occurring in Bone Metabolism and New Potential Treatment Strategies. International journal of molecular sciences. 2024 Oct 30;25(21):11639.

Calculators

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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.

Bioz

Keywords

MOQ

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100 mg

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

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DS37571084

All PTHR Isoforms