PF-3774076

CAT: 0804-HY-137055Size: 1 EachDry Ice: NoHazardous: No

1 / 1

CAT#:0804-HY-137055Size:1 Each

Selected

24/48H Stock Items & 2 to 6 Weeks non Stock Items.

Quick Request Actions

Description

PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.

CAS Number

1171824-96-6

UNSPSC

12352005

Hazard Statement

H301

Target

Adrenergic Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Others

Assay Protocol

https://www.medchemexpress.com/pf-3774076.html

Smiles

COCC1=C(Cl)C=CC2=C1CC[C@H]2C3=NC=CN3

Molecular Formula

C14H15ClN2O

Molecular Weight

262.73

Precautions

P264-P270-P330-P405-P501

References & Citations

[1]Pharmacological Properties of 2- ((R-5-Chloro-4-methoxymethyl indan-1-yl) -1H-imidazole (PF-3774076), a Novel and Selective 1A-Adrenergic Partial Agonist, in in Vitro and in Vivo Models of Urethral Function

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Related Products

Catalog	Name
HY-P991569	PF-04840082
HY-120689-01	PF-04745637
HY-160603-01	PF-05214030
HY-101383-01	PF-01247324
HY-12883A-01	PF-05198007
HY-15773-01	PF-4708671
HY-120072-01	PF-3450074
HY-100873-01	PF-1355
HY-119190-01	PF-06445974
HY-111371-01	PF-05180999

Alternative Products

Catalog	Name
WWB82496-01	PF-3774076
MBS579460	PF-03084014 (PF-3084014)
M36412-01	PF-17
M34376-01	PF-184298
M33060-01	PF-04957325
M28021-01	PF-1355
M26783-01	PF-04937319
M26368-01	PF-04885614
M24156-01	PF-9363
M23628-01	PF-06424439

PF-3774076

Related Products

Alternative Products

Popular Products