Motolimod (Synonyms: VTX-2337; VTX-378)

Name: Motolimod
Brand: MedChemExpress
SKU: HY-13773
Rating: 5.0 (9 reviews)

Cat. No.: HY-13773 Purity: 98.12%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC₅₀ of approximately 100 nM.

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

Motolimod Chemical Structure

CAS No. : 926927-61-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 166	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 166	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 784	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1176	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		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 9 publication(s) in Google Scholar

8 Publications Citing Use of MCE Motolimod

: Motolimod purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2017 Feb 17;292(7):2805-2814. [Abstract]; IL-1β ELISAs of supernatants from THP1 that are pre-incubated with medium or the indicated TLR8 agonists CL075 (5 μg/mL) or VTX-2337 (10 μM) for 16 h and after 8 h incubation in TLR8 agonist-free medium stimulated with 0.5 mg/mL ABC or medium for additional 16 h, respectively.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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

View All Isoforms

TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC₅₀ of approximately 100 nM.

IC₅₀ & Target

TLR8

In Vitro

Among the TLRs tested (TLR2, 3, 4, 5, 7, 8, and 9), Motolimod (VTX-2337) selectively activates TLR8. Motolimod stimulates the production of both TNFα (EC₅₀=140±30 nM based on 10 donors) and IL-12 (EC₅₀=120±30 nM based on 10 donors) in PBMCs. The EC₅₀ value for MIP-1β induction is 60 nM for Motolimod^[1].

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

In Vivo

Monkeys receive a subcutaneous injection of Motolimod (1 or 10 mg/kg), and plasma is collected predose, 6, 12, 24, and 96 h post-injection. For the 10 mg/kg dose, mean plasma levels of IL-1β increase from baseline levels of 0.5 pg/mL, up to 9.12±2.7 ng/mL (p<0.05, t-test) at 6 h post-administration of Motolimod (10 mg/kg). Circulating levels of IL-18 also increase from a baseline of ~ 1 pg/mL to 68.7±4.4 pg/mL (p<0.05, t-test) at 6 h in response to the Motolimod (VTX-2337) treatment (10 mg/kg). Levels of IL-6 are monitored, as this mediator is induced in response to TLR8 activation, but the release is independent of NLRP3 inflammasome activation. In addition, plasma levels of IFNγ are assessed as a measure of NK cell activation in response to Motolimod treatment^[2].

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

Clinical Trial

Molecular Weight

458.60

Formula

C₂₈H₃₄N₄O₂

CAS No.

926927-61-9

Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(C1=CC2=CC=C(C3=CC=C(C(N4CCCC4)=O)C=C3)C=C2N=C(N)C1)N(CCC)CCC

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 (109.03 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	2.1805 mL	10.9027 mL	21.8055 mL
5 mM	0.4361 mL	2.1805 mL	4.3611 mL
10 mM	0.2181 mL	1.0903 mL	2.1805 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 (5.45 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 (5.45 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 (5.45 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: 98.12%

Select Batch:

Data Sheet (280 KB) SDS (394 KB)

COA (250 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Lu H, et al. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509. [Content Brief]

[2]. Dietsch GN, et al. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity. PLoS One. 2016 Feb 29;11(2):e0148764. [Content Brief]

Kinase Assay ^[1]	Human embryonic kidney cells (HEK293) expressing TLR2, 3, 4, 5, 7, 8, or 9 are cultured in Dulbecco's Modified Eagle's Media containing 4.5 g/L L-glucose and 10% FBS. The activity of specific TLR agonists is assessed using the secretory embryonic alkaline phosphatase (SEAP) reporter gene that is linked to NF-κB activation in response to TLR stimulation. Measurement of SEAP activity using the Quanti-blue substrate after TLR agonist treatment is carried out similarly^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	PBMCs or purified NK cells are prepared, and the purity of NK cells is approximately 99%. NK cell-mediated cytotoxicity is assessed by Calcein AM release from labeled target cells. In brief, PBMCs or purified NK cells are cultured for 48 hours in RPMI medium in the presence of Motolimod (167 or 500 nM) before incubation with target cells^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Monkeys^[2] The male monkeys (2.9-4.9 kg) are housed individually (cage dimensions of 0.76 m wide×0.74 m deep×0.81 m in height), but commingled periodically as part of the environmental enrichment program. The animals are also given fruit, vegetable, or additional supplements as a form of environmental enrichment, as well as given various cage enrichment devices. Animals are given Certified Primate Diet, two times daily and water ad libitum. Motolimod is administered as a bolus subcutaneous (SC) injection in the intrascapular area at doses of 1 and 10 mg/kg. Blood samples are collected at baseline (pre-dose), and 6, 12, 24, and 96 h post injection to monitor levels of IL-1β and IL-18 in the plasma using the human MAP v.1.6 inflammation panel. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Lu H, et al. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509. [Content Brief] [2]. Dietsch GN, et al. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity. PLoS One. 2016 Feb 29;11(2):e0148764. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1805 mL	10.9027 mL	21.8055 mL	54.5137 mL
	5 mM	0.4361 mL	2.1805 mL	4.3611 mL	10.9027 mL
	10 mM	0.2181 mL	1.0903 mL	2.1805 mL	5.4514 mL
	15 mM	0.1454 mL	0.7268 mL	1.4537 mL	3.6342 mL
	20 mM	0.1090 mL	0.5451 mL	1.0903 mL	2.7257 mL
	25 mM	0.0872 mL	0.4361 mL	0.8722 mL	2.1805 mL
	30 mM	0.0727 mL	0.3634 mL	0.7268 mL	1.8171 mL
	40 mM	0.0545 mL	0.2726 mL	0.5451 mL	1.3628 mL
	50 mM	0.0436 mL	0.2181 mL	0.4361 mL	1.0903 mL
	60 mM	0.0363 mL	0.1817 mL	0.3634 mL	0.9086 mL
	80 mM	0.0273 mL	0.1363 mL	0.2726 mL	0.6814 mL
	100 mM	0.0218 mL	0.1090 mL	0.2181 mL	0.5451 mL

Motolimod 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:

Motolimod926927-61-9VTX-2337 VTX-378VTX2337VTX 2337VTX378VTX 378VTX-378Toll-like Receptor (TLR)Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

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.

Motolimod (Synonyms: VTX-2337; VTX-378)

Customer Review

Motolimod Related Antibodies

8 Publications Citing Use of MCE Motolimod

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

Motolimod Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Motolimod Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report