1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. KP136

KP136 (AL136) is an orally effective antiallergic agent. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation.

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

KP136 Chemical Structure

KP136 Chemical Structure

CAS No. : 76239-32-2

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Description

KP136 (AL136) is an orally effective antiallergic agent. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation[1].

IC50 & Target

Histamine release[1]

In Vitro

KP136 (0.01 μg/mL) inhibits this histamine release and degranulation in a dose-dependent manner, confirming that it is an inhibitor of mast cell activation. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation[1].

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

In Vivo

C4C at 0.2 mg/kg produces an equipotent effect to 1 mg/kg KP136 (KP-136) or 5 mg/kg DSCG. However, C4C is less effective by the oral route because it only produces a maximum inhibition of about 35% even at the high dose of 100 mg/kg, whereas KP136 shows an overt inhibitory effect of about 66% at the oral dose of 2 mg/kg. On the other hand, KP136 (1 mg/kg, i.v.) also remarkably inhibits 5-h homologous PCA, having an activity similar to that of C4C[1].

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

Molecular Weight

314.34

Formula

C16H18N4O3

CAS No.
SMILES

O=C1C(C2=NNN=N2)=CC3=CC=CC(OCCCCCC)=C3O1

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
Animal Administration
[1]

Pigs[1]
The trachea is taken from male guinea pigs, weighing 500-590 g, that are sacrificed by bleeding and then cut into 1.5 mm wide to make tracheal rings. Five specimens are tied at cartilage sites crossing each smooth muscle layer. This preparation is incubated in Tyrode's solution at 37°C, which is bubbled with 95% O2/5% CO2. The tension change of the tracheal muscle preparation is recorded through an isotonic transducer. C4C and KP136 in 0.5% KHCO3 or isoproterenol in saline is added cumulatively to the Tyrode's solution at a 1/200 volume. Relaxation percentage is calculated from the maximum relaxation value (100%) produces by re placement of the bathing medium with Tyrode's solution containing no CaCl2.

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

References
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    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.

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KP136
Cat. No.:
HY-U00168
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