2. Immunology/Inflammation
  3. Complement System
  4. JR14a

JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation.

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JR14a Chemical Structure

JR14a Chemical Structure

CAS No. : 2411440-41-8

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Based on 2 publication(s) in Google Scholar

JR14a Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation[1].

IC50 & Target

human complement C3a receptor[1]
Cellular Effect
Cell Line Type Value Description References
LAD2 IC50
8 nM
Compound: 14a; JR14a
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
[PMID: 31910011]
In Vitro

JR14a (0.1 nM-100 μM) inhibits C3a-induced intracellular Ca2+ release in human monocyte-derived macrophages, with an IC50 of 10 nM[1].
JR14a (0.1 nM-100 μM) is metabolically stable to exposure over 1 h to rat liver microsomes[1].
JR14a (0.1 nM-100 μM) inhibits C3a-induced β-hexosaminidase secretion in human LAD2 mast cells, with an IC50 of 8 nM[1].

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

JR14a Related Antibodies
In Vivo

JR14a (10 mg/kg; p.o. 2 h prior) reduces paw swelling by 65% over control at 30 min after agonist injection in acute rat paw model of inflammation and edema[1].
JR14a (1 mg/kg; i.v.) exhibits elimination half-life (191 min), clearance (4.4 mL/min/kg) and AUC (3795 ng h/mL) in rats[1].
JR14a (10 mg/kg; p.o.) exhibits Cmax (88 ng/mL), Tmax (300 min) and AUC (478 ng h/mL) in rats[1].

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

Animal Model: Male Wister rats (8 weeks, 250-300 g) were injected with BR103[1]
Dosage: 10 mg/kg
Administration: P.o. 2 h prior to agonist challenge
Result: Inhibited C3aR-mediated inflammation.
Animal Model: Male Wister rats (8 weeks, 250-300 g)[1]
Dosage: 1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: I.v.: t1/2=191 min, clearance=4.4 mL/min/kg, AUC=3795 ng•h/mL.
P.o.: Cmax=88 ng/mL, Tmax=300 min, AUC=478 ng•h/mL.
Molecular Weight

533.47

Formula

C25H26Cl2N4O3S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C(SC(C(C(C=C1)=CC=C1Cl)C(C=C2)=CC=C2Cl)=C3)=C3C)N[C@H](C(O)=O)CCCNC(N)=N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (93.73 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8745 mL 9.3726 mL 18.7452 mL
5 mM 0.3749 mL 1.8745 mL 3.7490 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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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 (4.69 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 (4.69 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 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: 99.59%

SDS (393 KB)

COA (250 KB) HNMR (262 KB) LCMS (94 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8745 mL 9.3726 mL 18.7452 mL 46.8630 mL
5 mM 0.3749 mL 1.8745 mL 3.7490 mL 9.3726 mL
10 mM 0.1875 mL 0.9373 mL 1.8745 mL 4.6863 mL
15 mM 0.1250 mL 0.6248 mL 1.2497 mL 3.1242 mL
20 mM 0.0937 mL 0.4686 mL 0.9373 mL 2.3431 mL
25 mM 0.0750 mL 0.3749 mL 0.7498 mL 1.8745 mL
30 mM 0.0625 mL 0.3124 mL 0.6248 mL 1.5621 mL
40 mM 0.0469 mL 0.2343 mL 0.4686 mL 1.1716 mL
50 mM 0.0375 mL 0.1875 mL 0.3749 mL 0.9373 mL
60 mM 0.0312 mL 0.1562 mL 0.3124 mL 0.7810 mL
80 mM 0.0234 mL 0.1172 mL 0.2343 mL 0.5858 mL
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JR14a 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:

JR14a2411440-41-8Complement SystemcomplementC3ainflammationInhibitorinhibitorinhibit

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