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

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.

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NDT 9513727 Chemical Structure

NDT 9513727 Chemical Structure

CAS No. : 439571-48-9

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Based on 1 publication(s) in Google Scholar

NDT 9513727 Related Antibodies

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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].

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

NDT 9513727 Related Antibodies
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].

MedChemExpress (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 (Pharmacokinetic Analysis)
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 (Pharmacokinetic Analysis)
Administration: Oral administration
Result: Oral bioavailability (26%), Cmax (830 nM), T1/2 (7.9 h).
Molecular Weight

573.68

Formula

C36H35N3O4
CAS No.
Appearance

Solid

Color

White to yellow

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
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (174.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 57 mg/mL (99.36 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7431 mL 8.7157 mL 17.4313 mL
5 mM 0.3486 mL 1.7431 mL 3.4863 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.36 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.35%

SDS (393 KB)

COA (261 KB) LCMS (108 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.7431 mL 8.7157 mL 17.4313 mL 43.5783 mL
5 mM 0.3486 mL 1.7431 mL 3.4863 mL 8.7157 mL
10 mM 0.1743 mL 0.8716 mL 1.7431 mL 4.3578 mL
15 mM 0.1162 mL 0.5810 mL 1.1621 mL 2.9052 mL
20 mM 0.0872 mL 0.4358 mL 0.8716 mL 2.1789 mL
25 mM 0.0697 mL 0.3486 mL 0.6973 mL 1.7431 mL
30 mM 0.0581 mL 0.2905 mL 0.5810 mL 1.4526 mL
40 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0895 mL
50 mM 0.0349 mL 0.1743 mL 0.3486 mL 0.8716 mL
60 mM 0.0291 mL 0.1453 mL 0.2905 mL 0.7263 mL
80 mM 0.0218 mL 0.1089 mL 0.2179 mL 0.5447 mL
DMSO 100 mM 0.0174 mL 0.0872 mL 0.1743 mL 0.4358 mL
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NDT 9513727 Related Classifications

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:

NDT 9513727439571-48-9NDT9513727NDT-9513727Complement SystemInhibitorinhibitorinhibit

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