SSR-240612 HCl

This product is for research use only, not for human use. We do not sell to patients.

SSR-240612 HCl
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Cat #: V3106 CAS #: 464930-42-5 Purity ≥ 98%

Description: SSR-240612 HCl, the hydrochloride salt of SSR240612, is a novel, potent, and orally bioactive specific non-peptide bradykinin B(1) receptor antagonist.

References: Gougat J, et al. SSR240612 [(2R)-2-[((3R)-3-(1,3-benzodioxol-5-yl)-3-[[(6-methoxy-2-naphthyl)sulfonyl]amino]propanoyl)amino]-3-(4-[[2R,6S)-2,6-dimethylpiperidinyl]methyl]phenyl)-N-isopropyl-N-methylpropanamide hydrochloride], a new nonpeptide antagonist o

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Molecular Weight (MW)793.42
Molecular FormulaC42H53ClN4O7S
CAS No.464930-42-5
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: ≥ 100 mg/mLr
Water: N/Ar
Ethanol: N/A
Solubility In VivoD-Phenylalaninamide, (3S)-3-(1,3-benzodioxol-5-yl)-N-((6-methoxy-2-naphthalenyl)sulfonyl)-beta-alanyl-4-(((2R,6S)-2,6-dimethyl-1-piperidinyl)methyl)-N-methyl-N-(1-methylethyl)-, hydrochloride (1:1)
SMILES CodeO=C(NC([C@@H](C1=CC=C(OCO2)C2=C1)CNS(=O)(C3=CC=C4C=C(OC)C=CC4=C3)=O)=O)[C@@H](CC5=CC=C(CN6[C@H](C)CCC[C@@H]6C)C=C5)N(C)C(C)C.[H]Cl
SynonymsSSR240612; SSR-240612 hydrochloride; SSR 240612; SSR240612 HCl
ProtocolIn VitroSSR240612 is a potent bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B2 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B1 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively. SSR240612 inhibits inositol phosphate 1 formation with an IC50 of 1.9 nM, but shows no obvious effect on inositol phosphate-1 formation induced by BK (3 nM) activation of B2 receptor in human fibroblast MRC5
In VivoSSR240612 (10 mg/kg p.o. or 0.3, 1 mg/kg i.p.) obviously blocks the des-Arg9-BK-induced paw edema in the mice. SSR240612 (10 and 30 mg/kg) reduces the duration of the late phase of paw licking in a dose dependent manner in the formalin model of inflammation in mice. SSR240612 (0.3, 3, and 30 mg/kg, p.o.) treatment before capsaicin potently and non-concentration-dependently reduces the ear edema. SSR240612 (0.3 mg/kg, i.v.) also suppresses the tissue destruction and neutrophil accumulation in the rat intestine, after splanchnic artery occlusion/reperfusion. Moreover, SSR240612 (1 and 3 mg/kg p.o.) dramacally increases the withdrawal latencies in the thermal hyperalgesia induced by UV irradiation in rats
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.2604 mL6.3018 mL12.6037 mL25.2073 mL
5mM0.2521 mL1.2604 mL2.5207 mL5.0415 mL
10mM0.1260 mL0.6302 mL1.2604 mL2.5207 mL
20mM0.0630 mL0.3151 mL0.6302 mL1.2604 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.