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-oxopyrrolidine-3-carboxamide Structure](CAS/20180723/GIF/1436004-46-4.gif)
- 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
- MSDS File:
- SDS
- TDS File:
- TDS
| 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) |  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 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0105423 | PA-9 99.73% | 1436004-46-4 | 1mg | $217 | 2026-06-04 | Buy |
| ChemScene | CS-0105423 | PA-9 99.73% | 1436004-46-4 | 5mg | $628 | 2026-06-04 | Buy |
| ChemScene | CS-0105423 | PA-9 99.73% | 1436004-46-4 | 10mg | $1246 | 2026-06-04 | Buy |
| ChemScene | CS-0105423 | PA-9 99.73% | 1436004-46-4 | 25mg | $2437 | 2026-06-04 | Buy |
| ChemScene | CS-0105423 | PA-9 99.73% | 1436004-46-4 | 50mg | $3792 | 2026-06-04 | Buy |
N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Chemical Properties, Uses, Production
Uses
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].
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].
in vivo
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].
| Animal Model: | Male ddY mice (6 weeks old at the start of experiments; intrathecal injection 100 pmol/5 μL PACAP)[1] |
| Dosage: | intrathecal injection, co-injection with PACAP. |
| Administration: | 100 pmol/5 μL |
| Result: | Attenuated the development of PACAP-induced aversive responses. Blocked the induction of PACAP-induced mechanical allodynia. |
IC 50
PAC1 receptor
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 | 32431 | 58 |
| Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 4000862158 18117107507 | vip@med-life.cn | China | 4999 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| TargetMol Chemicals Inc. | 13564774135 | marketing@targetmol.com | United States | 19950 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 58 |
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
