Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.

Product information

CAS Number: 69014-14-8

Molecular Weight: 312.42

Formula: C10H16N8S2

Chemical Name: N''-{4-[({2-[(Z)-N'-cyano-N''-methylcarbamimidamido]ethyl}sulfanyl)methyl]-1,3-thiazol-2-yl}guanidine

Smiles: C/N=C(/NCCSCC1=CSC(N=C(N)N)=N1)\NC#N

InChiKey: YDDXVAXDYKBWDX-UHFFFAOYSA-N

InChi: InChI=1S/C10H16N8S2/c1-14-9(16-6-11)15-2-3-19-4-7-5-20-10(17-7)18-8(12)13/h5H,2-4H2,1H3,(H2,14,15,16)(H4,12,13,17,18)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 125 mg/mL (400.10 mM; Need ultrasonic).

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:

Tiotidine competitively antagonizes the positive chronotropic action of histamine with an apparent dissociation constant of 30 μM (23-38 μM). Tiotidine abolishes H2-mediated increases in contractile force leaving H2-mediated negative inotropic responses unopposed. The actions of histamine at the A-V node, manifested by lengthening of the P-R interval and A-V block, are attenuated by 2.5 x 10(-7) M Tiotidine. Tiotidine actually behaves as an inverse agonist in U-937 cells, diminishing basal cAMP levels.

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