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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.

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CAS No.: 2460353-87-9
화학식: C₂₈H₃₀Cl₂N₄O₂
분자량:525.47

보관:

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

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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
분자량 525.47
화학식 C₂₈H₃₀Cl₂N₄O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

DS37571084

All PTHR Isoforms