OPC 21268 Chemical Properties

Boiling point:

772.5±60.0 °C(Predicted)

Density 

1?+-.0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: ≥20mg/mL

pka

16.17±0.46(Predicted)

form 

powder

color 

white to off-white

Safety Information

Hazard Codes 

Xn,N

Risk Statements 

22-50

Safety Statements 

61

RIDADR 

UN 3077 9 / PGIII

WGK Germany 

3

OPC 21268 Usage And Synthesis

Description

OPC 21268 is a nonpeptide antagonist of vasopressin V₁ receptors (IC₅₀ = 0.4 μM in rat liver membranes). It is selective for V₁ over V₂ receptors (IC₅₀ = >100 μM in kidney membranes). It is also selective for rat over human V₁ receptors (K_is = 25 and 8,800 nM, respectively), which can be partially attributed to the alanine residue at position 337 of the rat sequence, instead of a glycine residue in the human sequence, with differences at positions 224, 310, and 324 also contributing. OPC 21268 (0.03-1 mg/kg, i.v.) inhibits pressor responses induced by arginine vasopressin (argipressin; ) in pithed rats and arginine vasopressin-induced vasoconstriction in conscious rats (ID₅₀ = 2 mg/kg). It induces hypotension in aged spontaneously hypertensive rats (SHRs) and stroke-prone SHRs when administered at a dose of 3 mg/kg.

Uses

OPC 21268 is a nonpeptide AVP (Vasopressin) Receptor V antagonist.

storage

Store at +4°C