1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Tiotidine

Tiotidine (Synonyms: ICI 125211)

Cat. No.: HY-101232 Purity: >99.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Tiotidine Chemical Structure

Tiotidine Chemical Structure

CAS No. : 69014-14-8

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10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
1 mg USD 85 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target[1]

H2 Receptor

7.3-7.8 (pA2)

H1 receptor

<4.5 (pA2)

H3 Receptor

4.8 (pA2)

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[2].
Tiotidine actually behaves as an inverse agonist in U-937 cells, diminishing basal cAMP levels[3].

Molecular Weight

312.42

Formula

C₁₀H₁₆N₈S₂

CAS No.

69014-14-8

SMILES

CN/C(NC#N)=N\CCSCC1=CSC(NC(N)=N)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

TiotidineICI 125211ICI125211ICI-125211Histamine ReceptorselectiveinverseagonistU-937cellscAMPhistamineInhibitorinhibitorinhibit

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Tiotidine
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