CU-CPT 4a (Synonyms: TLR3-IN-1)

Name: CU-CPT 4a
Brand: MedChemExpress
SKU: HY-108473
Rating: 5.0 (12 reviews)

Cat. No.: HY-108473 Purity: 99.50%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

CU-CPT 4a (TLR3-IN-1) is a potent, highly selective TLR3 signaling inhibitor. CU-CPT 4a represses the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-α and IL-1β.

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

CAS No. : 1279713-77-7

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
200 mg	Get quote
500 mg	Get quote

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

Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of CU-CPT 4a:

CU-CPT 4a (Standard) Get quote

12 Publications Citing Use of MCE CU-CPT 4a

Cell Imaging/Staining

In Vivo Efficacy Study

Histological Imaging/Staining

ELISA

: CU-CPT 4a purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 May;14(5):e70083. [Abstract]; m6A levels in EVs regulate inflammatory responses via TLR8 in macrophages. Differentiated THP‐1 cells (dTHP‐1) were pretreated with or without CU‐CPT‐9a (HY-112667; 48 h) and CU‐CPT‐4a (HY-108473; 48 h). Whole‐cell lysates obtained from dTHP‐1 cells were subjected to Western blot analysis using an anti‐phospho p65 antibody, anti‐p65 antibody and anti‐β‐actin antibody. Representative images from three independent experiments are shown.

: CU-CPT 4a purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 May;14(5):e70083. [Abstract]; m6A levels in EVs regulate inflammatory responses via TLR8 in macrophages. Differentiated THP‐1 cells (dTHP‐1) were pretreated with or without CU‐CPT‐9a (HY-112667; 48 h) and CU‐CPT‐4a (HY-108473; 48 h). Conditioned medium from dTHP‐1 cells treated with CCD‐841‐CoN or HT29 small EVs was used for ELISA. dTHP‐1 cells were pre‐transfected with or without TLR8 siRNA.

: CU-CPT 4a purchased from MedChemExpress. Usage Cited in: Mol Pain. 2025 May 23:17448069251346373. [Abstract]; TLR3 antagonist CU CPT4a inhibited NTG-induced mechanical allodynia. Repeated treatment with CU CPT4a (5 mg/kg, i.p.) or vehicle (equal volumes of DMSO) every other day before NTG injections for 9 days. Repeated treatment with CU CPT4a inhibited basal hind paw mechanical and periorbital mechanical allodynia.

: CU-CPT 4a purchased from MedChemExpress. Usage Cited in: Mol Pain. 2025 May 23:17448069251346373. [Abstract]; TLR3 antagonist CU CPT4a inhibited NTG-induced mechanical allodynia. Repeated treatment with CU CPT4a (5 mg/kg, i.p.) or vehicle (equal volumes of DMSO) every other day before NTG injections for 9 days. Post-treatment responses, including hind paw mechanical and periorbital mechanical allodynia, were estimated 2 h after NTG administration.

: CU-CPT 4a purchased from MedChemExpress. Usage Cited in: Mol Pain. 2025 May 23:17448069251346373. [Abstract]; TLR3 antagonist CU CPT4a (5 mg/kg; i.p.; every other day for 9 days before NTG injection) reduced the expression of TLR3 in TNC. Quantitative analysis of the number of TLR3+Neuron in the TNC in a 212 × 212 µm² visual field of each section per mouse after NTG injection.

: CU-CPT 4a purchased from MedChemExpress. Usage Cited in: Mol Pain. 2025 May 23:17448069251346373. [Abstract]; TLR3 antagonist CU CPT4a (5 mg/kg; i.p.; every other day for 9 days before NTG injection) reduced the expression of TLR3 in TNC. Immunoblot analysis of TLR3 (n = 5).

: CU-CPT 4a purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Nov 3;14(1):7048. [Abstract]; Immunofluorescence images of MMP21 in the absence or presence of RIG012 or CU-CPT 4a. β-cat ΔN/RasV12 cells were mixed with β-cat ΔN cells in the presence of BFA, and were treated with DMSO, 2.5 μM RIG012 or 50 μM CU-CPT 4a. Cells were stained with Hoechst 33342 (blue) and anti-MMP21 antibody (white).

: CU-CPT 4a purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Nov 3;14(1):7048. [Abstract]; Immunofluorescence images of MMP21 or p65 in intestinal organoids from APCMin-Villin-RasV12 mice in the absence or presence of 10 μM RIG012 or 100 μM CU-CPT 4a.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

TLR3

3.44 μM (IC₅₀, in RAW 264.7 cells)

In Vitro

CU-CPT 4a shows dose-dependent inhibitory effects blocking Poly (I:C)-induced TLR3 activation with an IC₅₀ of 3.44 μM^[1].
CU-CPT 4a competes with dsRNA for binding to TLR3 with a K_i of 2.96 μM^[1].

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

Molecular Weight

377.82

Formula

C₁₈H₁₃ClFNO₃S

CAS No.

1279713-77-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)[C@@H](CC1=CC=CC=C1)NC(C2=C(Cl)C3=CC=C(F)C=C3S2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (264.68 mM; Need ultrasonic; 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	2.6468 mL	13.2338 mL	26.4676 mL
5 mM	0.5294 mL	2.6468 mL	5.2935 mL
10 mM	0.2647 mL	1.3234 mL	2.6468 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)

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 (6.62 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.

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: 99.50%

Select Batch:

Data Sheet (276 KB) SDS (254 KB)

COA (248 KB) RP-HPLC (221 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Yibo Wang, et al. Small-Molecule Modulators of Toll-like Receptors. Acc Chem Res. 2020 May 19;53(5):1046-1055. [Content Brief]

Cell Assay
^[1]

RAW 264.7 cells are planted in 6-well plates in duplicate at 1,000,000 cells per well with 3 mL of medium (RPMI 1640 medium, supplemented with 10% FBS, Penicillin (100 U/mL) and Streptomycin (100 mg/mL)) and grown for 24 h at 37°C in a 5% CO₂ humidified incubator. After 24 h, non-adherent cells and media are removed and replaced with fresh RPMI 1640 medium (3 mL/well). Two wells of adherent macrophages are treated with Poly (I:C) (15 μg/mL). One of the two wells is treated with 27 μM CU CPT 4a. One additional well is treated with only CU CPT 4a (27 μM) only. Plates are then incubated for an additional 24 h. After removal of the medium, cells are washed with PBS (3×1 mL), the 6 well plate is put on ice, then 500 μL of lysis buffer is added in each well (Lysis Buffer: 120 μL 0.5M EDTA; 12 mL Mammalian Protein Extraction Reagent, 100 μL cocktail, 0.36 mL NaCl (5 M, aqueous) ). After 5 min, the mixture is transferred into corresponding 1.5 mL tube, spun for 20 min at 13.2 K rpm in a cold room. Approximately 400 μL of supernatant are collected into new tubes, frozen at -80°C until ready for cytokine measurement^[1].

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

References

[1]. Yibo Wang, et al. Small-Molecule Modulators of Toll-like Receptors. Acc Chem Res. 2020 May 19;53(5):1046-1055. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6468 mL	13.2338 mL	26.4676 mL	66.1691 mL
	5 mM	0.5294 mL	2.6468 mL	5.2935 mL	13.2338 mL
	10 mM	0.2647 mL	1.3234 mL	2.6468 mL	6.6169 mL
	15 mM	0.1765 mL	0.8823 mL	1.7645 mL	4.4113 mL
	20 mM	0.1323 mL	0.6617 mL	1.3234 mL	3.3085 mL
	25 mM	0.1059 mL	0.5294 mL	1.0587 mL	2.6468 mL
	30 mM	0.0882 mL	0.4411 mL	0.8823 mL	2.2056 mL
	40 mM	0.0662 mL	0.3308 mL	0.6617 mL	1.6542 mL
	50 mM	0.0529 mL	0.2647 mL	0.5294 mL	1.3234 mL
	60 mM	0.0441 mL	0.2206 mL	0.4411 mL	1.1028 mL
	80 mM	0.0331 mL	0.1654 mL	0.3308 mL	0.8271 mL
	100 mM	0.0265 mL	0.1323 mL	0.2647 mL	0.6617 mL

CU-CPT 4a 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:

CU-CPT 4a1279713-77-7TLR3-IN-1Toll-like Receptor (TLR)TLR3/dsRNA complexTNF-αIL-1βprotein-RNA interactionInhibitorinhibitorinhibit

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CU-CPT 4a (Synonyms: TLR3-IN-1)

Customer Review

Other Forms of CU-CPT 4a:

CU-CPT 4a Related Antibodies

12 Publications Citing Use of MCE CU-CPT 4a

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Toll-like Receptor (TLR) Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

CU-CPT 4a Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CU-CPT 4a Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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