1. Immunology/Inflammation
  2. Complement System
  3. NDT 9513727

NDT 9513727 

Cat. No.: HY-110060 Purity: ≥99.0%
Handling Instructions

NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with an IC50 of 11.6 nM. NDT 9513727 can be used for the research of human inflammatory diseases.

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

NDT 9513727 Chemical Structure

NDT 9513727 Chemical Structure

CAS No. : 439571-48-9

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10 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with an IC50 of 11.6 nM. NDT 9513727 can be used for the research of human inflammatory diseases[1].

IC50 & Target

IC50: 11.6 nM (human C5aR)[1]

In Vitro

NDT 9513727 inhibits C5a-stimulated responses, including guanosine 5'-3-O-(thio)triphosphate binding, Ca2+ mobilization, oxidative burst, degranulation, cell surface CD11b expression and chemotaxis in various cell types with IC50s from 1.1 to 9.2 nM, respectively[1].

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

In Vivo

NDT 9513727 (3-30 mg/kg; p.o.) exhibits a dose-dependent inhibition of hC5a-induced neutropenia[1].
NDT 9513727 exhibits moderate oral bioavailability (rat 73%, monkey 26%) and Cmax (rat 5.98 μM, monkey 830 nM) following oral administration (rat 50, monkey 25.2 mg/kg)[1].
NDT 9513727 exhibits moderate plasma elimination half-lives (rat 4.8, monkey 7.9 h) due to low plasma clearance (1.4 L/h/kg and 3.8 l/h/kg respectively) following oral administration (rat 50, monkey 25.2 mg/kg)[1].

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

Animal Model: Six-week-old Mongolian gerbils[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration
Result: Significantly inhibited hC5a-induced neutropenia at 3 mg/kg, 10 mg/kg, 30 mg/kg.
Animal Model: Rat[1]
Dosage: 50 mg/kg
Administration: Oral administration
Result: Oral bioavailability (73%), Cmax (5.98 μM), T1/2 (4.8 h).
Animal Model: Monkey[1]
Dosage: 25.2 mg/kg
Administration: Oral administration
Result: Oral bioavailability (26%), Cmax (830 nM), T1/2 (7.9 h).
Molecular Weight

573.68

Formula

C₃₆H₃₅N₃O₄

CAS No.

439571-48-9

SMILES

CCCCN1C(CN(CC2=CC=C(OCO3)C3=C2)CC4=CC=C(OCO5)C5=C4)=C(C6=CC=CC=C6)N=C1C7=CC=CC=C7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: ≥99.0%

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Keywords:

NDT 9513727NDT9513727NDT-9513727Complement SystemInhibitorinhibitorinhibit

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NDT 9513727
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