CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.

Product information

CAS Number: 191672-52-3

Molecular Weight: 673.65

Formula: C34H38Cl2N2O6S

Chemical Name: (2S)-1'-{2-[(2R)-2-(3,4-dichlorophenyl)-4-(3,4,5-trimethoxybenzoyl)morpholin-2-yl]ethyl}-3H-spiro[2λ⁴-benzothiophene-1,4'-piperidin]-2-one

Smiles: COC1C=C(C=C(OC)C=1OC)C(=O)N1C[C@](CCN2CCC3(CC2)C2=CC=CC=C2C[S@@]3=O)(OCC1)C1C=C(Cl)C(Cl)=CC=1

InChiKey: RWSBBXFLRGQFQP-RKCQUONGSA-N

InChi: InChI=1S/C34H38Cl2N2O6S/c1-41-29-18-24(19-30(42-2)31(29)43-3)32(39)38-16-17-44-33(22-38,25-8-9-27(35)28(36)20-25)10-13-37-14-11-34(12-15-37)26-7-5-4-6-23(26)21-45(34)40/h4-9,18-20H,10-17,21-22H2,1-3H3/t33-,45-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

CS-003 (0.01-10 μM; 24 hours) inhibits NK1, NK2 or NK3 induced inositol phosphate formation in a concentration-dependent manner with pA2 values of 8.7, 9.4 and 9.5 μM, respectively.

In Vivo:

CS-003 (intravenous injection; 0.01-3.0 mg/kg; 5 min before neurokinin A/B/C injection) inhibits substance P-induced tracheal vascular hyperpermeability, neurokinin A- and neurokinin B-induced bronchoconstriction with ID50 values of 0.13, 0.040 and 0.063 mg/kg, respectively.

Products are for research use only. Not for human use.