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N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide

CAS No.
1436004-46-4
Chemical Name:
N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide
Synonyms
N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide;3-Pyrrolidinecarboxamide, N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxo-;N-?[2-?(1H-Imidazol-?5-?yl)?ethyl]?-?1-?(1H-?indazol-?3-?yl)?-?5-?oxo-3-?pyrrolidinecarboxami?de
CBNumber:
CB54567830
Molecular Formula:
C17H18N6O2
Molecular Weight:
338.36
MDL Number:
MFCD23139263
MOL File:
1436004-46-4.mol
Last updated:2024-07-02 08:55:11

N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Properties

Boiling point 880.0±65.0 °C(Predicted)
Density 1.440±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : 250 mg/mL (738.86 mM; Need ultrasonic)
pka 13.33±0.40(Predicted)
form Solid
color White to light yellow

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H335-H319
Precautionary statements  P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362

N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Chemical Properties,Uses,Production

Biological Activity

PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain[1]. PA-9 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP-induced (1 nM) CREB phosphorylation in the CHO cells expressing PAC1 receptors[1]. PA-9 (100 pmol; co-injection with PACAP) attenuates the development of PACAP-induced (100 pmol/5 μL; intrathecal injection) aversive responses of mice[1].PA-9 (100 pmol; co-injection with PACAP) significantly blocks the induction of PACAP-induced (100 pmol) mechanical allodynia[1].PA-9 (100 pmol/5 μl; single intrathecal injection alone) does not induce aversive responses and mechanical allodynia of mice[1].PA-9 is well accommodated in the subpocket formed by L80, F81, I83, G91, V92, P107, A112, and C113 of the PAC1 receptor, precipitating in hydrophobic interactions[1].

References

[1]. Takasaki I, et al. In Silico Screening Identified Novel Small-molecule Antagonists of PAC1 Receptor. J Pharmacol Exp Ther. 2018 Apr;365(1):1-8.

N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Preparation Products And Raw materials

Raw materials

Preparation Products

N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Suppliers

Global( 6)Suppliers
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
TargetMol Chemicals Inc. 4008200310 marketing@tsbiochem.com China 23980 58
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd 021-59167510 18117107507 vip@med-life.cn China 5012 58
N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide N-?[2-?(1H-Imidazol-?5-?yl)?ethyl]?-?1-?(1H-?indazol-?3-?yl)?-?5-?oxo-3-?pyrrolidinecarboxami?de 3-Pyrrolidinecarboxamide, N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxo- 1436004-46-4