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
Boiling point | 880.0±65.0 °C(Predicted) |
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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) | 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
Supplier | Tel | 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 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
TargetMol Chemicals Inc. | 58 |
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 58 |