2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor mAChR
  4. HY-078020

HY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC50 of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases.

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HY-078020 Chemical Structure

HY-078020 Chemical Structure

CAS No. : 2756222-90-7

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HY-078020 Related Antibodies

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Description

HY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC50 of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases[1].

IC50 & Target

H1 Receptor

24.12 nM (IC50)

mAChR3

 

In Vitro

HY-078020 reveals a potent inhibitory activity towards H1R (IC50 is 24.12 nM) and weak inhibition against M3R and hERG, with IC50s of >10 and 17.6 μM, respectively[1].
HY-078020 exhibits moderate permeability (efflux ratio rate <2), liver microsomes stability with long half-life in human, beagles and mice (T1/2 = 86.625 min) [1].
HY-078020 exhibits inhibitory activity against cytochrome P450 (CYP) isozymes CYP3A4 of rates[1].

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

HY-078020 Related Antibodies
In Vivo

HY-078020 (5 mg/kg, i.g.) inhibits the histamine induced skin vasodilation and capillary permeability in ICR/KM mice, with a vascular permeability inhibition rates of 58.71 %[1].
HY-078020 (10 mg/kg, i.v.) exhibits aweak anticholinergic activity with an inhibition rate of salivary secretion of 10.8% in Wistar mice[1].
HY-078020 reveals a pharmacokinetic profils in mice[1]:

Pharmacokinetic Analysis of HY-078020 in wistar male rats[1]

route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-inf (ng·h/mL) Vd (L/kg) CL (mL/h/kg) MRT0-inf(h) F (%)
iv 4 0.653 ± 0.12 - - 1678 ± 152.59 1822.38 ± 224.97 1.77 ± 0.22 37.00 ± 4.62 0.70 ± 0.14 59.55
po 25 4.05 ± 0.81 0.38 ± 0.16 1722.06 ± 337.11 6246.92 ± 1443.28 7209.70 ± 1419.01 21.26 ± 7.42 59.35 ± 10.59 6.01 ± 1.42 -

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

Animal Model: histamine-induced vascular permeability in ICR and Kunming mice[1]
Dosage: 5 mg/kg
Administration: i.g.
Result: Reduced the vascular permeability with an inhibition rate of 58.71%.
Animal Model: Wistar mice[1]
Dosage: 10 mg/kg
Administration: i.v., once a day
Result: Inhibited salivary secretion with an inhibition rate of 10.8%.
Molecular Weight

515.09

Formula

C32H35ClN2O2
CAS No.
SMILES

ClC(C=C1)=CC(CCC2=C/3N=CC=C2)=C1C3=C4CCN(CCCC5=CC(C(C)(C(O)=O)C)=CC=C5)CC/4
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
References
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HY-078020 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HY-0780202756222-90-7HY078020HY 078020Histamine ReceptormAChRMuscarinic acetylcholine receptorallergic diseaseanticholinergicantihistamineInhibitorinhibitorinhibit

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