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Cat. No.: HY-189807

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GD136

Name: GD136
Brand: MedChemExpress
SKU: HY-189807
Availability: PreOrder

(Synonyms: VUF10775)

GD136 (VUF10775) is a histamine H1/H4 receptor antagonist that blocks histamine signaling. The pK_i of GD136 for H1 is 7.61 (human), 7.80 (mouse), and 7.44 (rat), and for H4 is 7.93 (human), 7.38 (mouse), 7.28 (rat), and 7.38 (monkey). GD136 alleviates ocular hyperemia. GD136 can be used in research on allergic conjunctivitis.

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

Formula: C₂₂H₂₆ClF₃N₆O₂S
Molecular Weight:530.99

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

GD136 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
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Bioz

Biological Activity

Description

IC₅₀ & Target

Human H₁ Receptor

7.61 (pKi)

Human H₄ Receptor

7.93 (pKi)

All Histamine Receptor Isoforms :

In Vitro

GD136 (35.HCl) binds to human H1R and H4R in HEK293T membrane radioligand binding assays, with pK_i values of 7.61 and 7.93, respectively^[1].
GD136 antagonizes human H1R and H4R in the CRE-luciferase reporter gene assay, with pK_b values of 6.25 and 7.19, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

Molecular Weight 530.99
Formula C₂₂H₂₆ClF₃N₆O₂S
SMILES

CN(CC1)CCN1C2=NC3=CC=CC(C(F)(F)F)=C3C(NCCS(NC4=CC=CC=C4)(=O)=O)=N2.Cl
Synonyms

VUF10775
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Weber P, et al. From Fragment Hit to Clinical Candidate: Discovery of Dual H1R/H4R Ligands with Superior Efficacy in Allergic Conjunctivitis. Journal of medicinal chemistry. 2026 Sep 10;69(17):20967-21003.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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GD136

All Histamine Receptor Isoforms