JR14a

Name: JR14a
Brand: MedChemExpress
SKU: HY-138161
Rating: 5.0 (8 reviews)

Cat. No.: HY-138161 Purity: 99.77%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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

CAS No. : 2411440-41-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	Get quote
10 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 8 publication(s) in Google Scholar

8 Publications Citing Use of MCE JR14a

RT-PCR

Cell Proliferation/Viability Assay

Cell Imaging/Staining

In Vivo Efficacy Study

Flow Cytometry

: JR14a purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2025 Apr 9:108500. [Abstract]; JR14a (C3aRA; 50, 100, 200, 300 nM; 48 h) shows 200 nM C3aRA on top of 100 mM D-gal intervention, the cell viability was significantly restored to a relatively desirable level, indicating that C3aRA has a protective effect against D-gal-induced cell damage at this concentration in MC3T3-E1 cells.

: JR14a purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2025 Apr 9:108500. [Abstract]; A-b-gal staining and quantitative analysis. MC3T3-E1 cells were cultured in media supplemented with D-gal (100 mM) or D-gal + C3aRA (JR14a, a novel antagonist of C3aR, 200 nM) for 48 h.

: JR14a purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2025 Apr 9:108500. [Abstract]; MC3T3-E1 cells were cultured in media supplemented with D-gal (100 mM) or D-gal + C3aRA (JR14a, a novel antagonist of C3aR, 200 nM) for 48 h. Flow cytometry analysis of apoptosis in the different groups.

: JR14a purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2025 Apr 9:108500. [Abstract]; MC3T3-E1 cells were cultured in media supplemented with D-gal (100 mM) or D-gal + C3aRA (JR14a, a novel antagonist of C3aR, 200 nM) for 48 h. Representative immunofluorescence images of C3aR, p53, p21, and p16 expression.

: JR14a purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2022 Sep;33(9):1742-1756. [Abstract]; Human podocytes were exposed to medium containing 10% MN plasma (with C3a 1966.76259.0 ng/ml), 10% MN plasma 1 C3aR antagonist SB290157, 10% MN plasma 1 C3aR antagonist JR14a, 10% MN plasma 1 human C3a (2 mg/ml), 10% healthy plasma, C3a, or blank control. The expression of PLA2R was significantly elevated after exposure to MN plasma, and blocked by C3aR antagonists JR14a (10, 20, 100, 200 nM).

: JR14a purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2022 Sep;33(9):1742-1756. [Abstract]; JR14a (20 nM; 72 h) arrested MN plasma induced a decrease in the viability of podocytes.

: JR14a purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2022 Sep;33(9):1742-1756. [Abstract]; JR14a (10 mg/kg; po; daily for 7 weeks) in Sprague-Dawley rats with Heymann nephritis (early-treatment group from day 0 ; the late-treatment group from day 21) alleviated plasma level of C3a.

: JR14a purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2022 Sep;33(9):1742-1756. [Abstract]; JR14a (10 mg/kg; po; daily for 7 weeks) in Sprague-Dawley rats with Heymann nephritis (early-treatment group from day 0 ; the late-treatment group from day 21) alleviated glomerular expression of C3aR.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

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.

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 C_max (88 ng/mL), T_max (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.: t_1/2=191 min, clearance=4.4 mL/min/kg, AUC=3795 ng•h/mL. P.o.: C_max=88 ng/mL, T_max=300 min, AUC=478 ng•h/mL.

Molecular Weight

533.47

Formula

C₂₅H₂₆Cl₂N₄O₃S

CAS No.

2411440-41-8

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
10 mM	0.1875 mL	0.9373 mL	1.8745 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (4.69 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 Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 5 mg/mL (9.37 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.77%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (250 KB) HNMR (183 KB) RP-HPLC (225 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Rowley JA, et, al. Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity. J Med Chem. 2020 Jan 23;63(2):529-541. [Content Brief]

Complete Stock Solution Preparation Table

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

JR14a Related Classifications

Inflammation/Immunology

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

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

JR14a

Customer Review

JR14a Related Antibodies

8 Publications Citing Use of MCE JR14a

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

JR14a Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

JR14a Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report