NCO-650 free base
NCO-650 free base is an antiallergic agent that acts by inhibiting tryptase, a key trypsin-like protease in mast cells. NCO-650 free base inhibits mast cell histamine release, increases intracellular cAMP levels in mast cells, suppresses bronchoconstriction, and prevents decreases in perfusion pressure and systemic blood pressure. NCO-650 free base is applicable to the research of allergic diseases and bronchial asthma.
For research use only. We do not sell to patients.
- CAS No.: 81907-78-0
- Formula: C19H29N3O2
- Molecular Weight:331.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
NCO-650 free base potently inhibits histamine release from rat peritoneal mast cells induced by antigen (IC50 = 1.9 μM), anti-IgE (IC50 = 3.6 μM), Concanavalin A (HY-P2149) (IC50 = 4.6 μM), Ionophore A23187 (HY-N6687) (IC50 = 2.9 μM), and Compound 48/80 (HY-115768) (IC50 = 6.1 μM) via dose-dependent action[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel (male, 8.5-18.5 kg, anesthetized, nonimmunologically induced bronchial asthma model)[3]
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Dosage:100 mg/kg
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Administration:i.d.; single dose
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Result:Produced a 64% inhibition of the maximal increase in ventilation overflow induced by compound 48/80.
Significantly inhibited the decreases in perfusion pressure and systemic blood pressure caused by compound 48/80.
Had no effect on ventilation overflow, perfusion pressure, or systemic blood pressure when administered alone.
Did not inhibit the increase in ventilation overflow induced by inhalation of 0.005-0.01% histamine for 10 min.
Chemical Information
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CAS No. 81907-78-0
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Molecular Weight 331.45
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Formula C19H29N3O2
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SMILES
O=C([C@H]1CC[C@@H](CC1)CNC(N)=N)OC2=CC=C(C=C2)C(C)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Takei M, et al. Inhibitory effect of anti-allergic agent NCO-650 on histamine release induced by various secretagogues. Agents Actions. 1988;25(1-2):17-21. [Content Brief]
[2]. Takei M, et al. Inhibition of cAMP increase by an anti-allergic agent, NCO-650, during histamine release. Int Arch Allergy Appl Immunol. 1989;88(4):377-380. [Content Brief]
[3]. Misawa M, et al. Effects of mast cell stabilizers on a new bronchial asthma model using compound 48/80 in dogs. Jpn J Pharmacol. 1987;44(2):197-205. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)