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
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.
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)