1191908-24-3

Name	3-Pyridinecarboxamide, 5-chloro-1-[(1R)-1-(3-cyanophenyl)ethyl]-1,2-dihydro-2-imino-
CAS	1191908-24-3
Molecular Formula	C15H13ClN4O
Molecular Weight	300.74
MOL File	1191908-24-3.mol

Synonyms

ADRA1D receptor antagonist 1 free base 3-Pyridinecarboxamide, 5-chloro-1-[(1R)-1-(3-cyanophenyl)ethyl]-1,2-dihydro-2-imino-

show less show more

Chemical Properties

Boiling point	450.1±55.0 °C(Predicted)
density	1.34±0.1 g/cm3(Predicted)
pka	13.45±0.20(Predicted)

Hazard Information

Uses

ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.

in vivo

ADRA1D receptor antagonist 1 (free base) (10 μg/kg; p.o.; single) inhibits cyclophosphamide-induced urinary frequency in rats^[1].
ADRA1D receptor antagonist 1 (free base) (4.4 μg/kg; i.v.; single) inhibits bladder contraction with an IC 30 value of 15 nM in rats^[1].

Animal Model:	Rats with cyclophosphamide-induced cystitis^[1].
Dosage:	10 μg/kg
Administration:	Oral administration; single
Result:	Increased voiding intervals.

Animal Model:	Rats with BOO (bladder outlet obstruction)^[1].
Dosage:	4.4 μg/kg
Administration:	Intravenous injection; single
Result:	Dose-dependently decreased the non-voiding bladder contractions during urinary storage phase.

References

[1] Sakauchi N, et al. Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities. J Med Chem. 2016 Apr 14;59(7):2989-3002. DOI:10.1021/acs.jmedchem.5b01528

Supplier

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

PROMPT×

PROMPT
The What'sApp is temporarily not supported in mainland China

Cancel

Determine

Send Inquriy