WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 203153
CAS#: 926927-61-9
Description: Motolimod, also known as VTX-2337, is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities. TLR8 agonist VTX-2337 binds to TLR8, present in cutaneous dendritic cells, monocytes/macrophages, and mast cells, which may result in the activation of the central transcription factor nuclear factor-B, the secretion of proinflammatory cytokines and other mediators, and a Th1-weighted antitumoral cellular immune response. Primarily localized to endosomal membranes intracellularly, TLR8, like other TLRs, recognizes pathogen-associated molecular patterns (PAMPs) and plays a key role in the innate immune system.
MedKoo Cat#: 203153
Name: Motolimod
CAS#: 926927-61-9
Chemical Formula: C28H34N4O2
Exact Mass: 458.2682
Molecular Weight: 458.606
Elemental Analysis: C, 73.33; H, 7.47; N, 12.22; O, 6.98
Synonym: VTX-2337; VTX 2337; VTX2337; Motolimod.
IUPAC/Chemical Name: 2-amino-N,N-dipropyl-8-(4-(pyrrolidine-1-carbonyl)phenyl)-3H-benzo[b]azepine-4-carboxamide
InChi Key: QSPOQCXMGPDIHI-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H34N4O2/c1-3-13-31(14-4-2)28(34)24-17-23-12-11-22(18-25(23)30-26(29)19-24)20-7-9-21(10-8-20)27(33)32-15-5-6-16-32/h7-12,17-18H,3-6,13-16,19H2,1-2H3,(H2,29,30)
SMILES Code: O=C(C1=CC2=CC=C(C3=CC=C(C(N4CCCC4)=O)C=C3)C=C2N=C(N)C1)N(CCC)CCC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM. |
| In vitro activity: | VTX-2337 selectively activates TLR8 with an EC(50) of about 100 nmol/L and stimulates production of TNFα and interleukin (IL)-12 from monocytes and myeloid dendritic cells (mDC). VTX-2337 stimulates IFNγ production from NK cells and increases the cytotoxicity of NK cells against K562 and ADCC by rituximab and trastuzumab. Reference: Clin Cancer Res. 2012 Jan 15;18(2):499-509. https://pubmed.ncbi.nlm.nih.gov/22128302/ |
| In vivo activity: | Intra-TG injection of the TLR8 agonist VTX-2337 induced pain hypersensitivity in mice. VTX-2337 also increased the intracellular Ca2+ concentration, induced the activation of ERK and p38, and increased the expression of pro-inflammatory cytokines in the TG. Reference: Neurosci Bull. 2021 Apr;37(4):550-562. https://pubmed.ncbi.nlm.nih.gov/33355900/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 26.0 | 56.69 | |
| DMSO:PBS (pH 7.2) (1:4) | 0.2 | 0.44 | |
| Ethanol | 15.0 | 32.71 |
The following data is based on the product molecular weight 458.606 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Dietsch GN, Lu H, Yang Y, Morishima C, Chow LQ, Disis ML, Hershberg RM. 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. doi: 10.1371/journal.pone.0148764. PMID: 26928328; PMCID: PMC4771163. 2. Lu H, Dietsch GN, Matthews MA, Yang Y, Ghanekar S, Inokuma M, Suni M, Maino VC, Henderson KE, Howbert JJ, Disis ML, Hershberg RM. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509. doi: 10.1158/1078-0432.CCR-11-1625. Epub 2011 Nov 29. PMID: 22128302. 3. Fu YY, Cen JK, Song HL, Song SY, Zhang ZJ, Lu HJ. Ginsenoside Rh2 Ameliorates Neuropathic Pain by inhibition of the miRNA21-TLR8-mitogen-activated protein kinase axis. Mol Pain. 2022 Apr;18:17448069221126078. doi: 10.1177/17448069221126078. PMID: 36039405; PMCID: PMC9478689. 4. Zhao LX, Jiang M, Bai XQ, Cao DL, Wu XB, Zhang J, Guo JS, Chen TT, Wang J, Wu H, Gao YJ, Zhang ZJ. TLR8 in the Trigeminal Ganglion Contributes to the Maintenance of Trigeminal Neuropathic Pain in Mice. Neurosci Bull. 2021 Apr;37(4):550-562. doi: 10.1007/s12264-020-00621-4. Epub 2020 Dec 23. PMID: 33355900; PMCID: PMC8055805. |
| In vitro protocol: | 1. Dietsch GN, Lu H, Yang Y, Morishima C, Chow LQ, Disis ML, Hershberg RM. 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. doi: 10.1371/journal.pone.0148764. PMID: 26928328; PMCID: PMC4771163. 2. Lu H, Dietsch GN, Matthews MA, Yang Y, Ghanekar S, Inokuma M, Suni M, Maino VC, Henderson KE, Howbert JJ, Disis ML, Hershberg RM. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509. doi: 10.1158/1078-0432.CCR-11-1625. Epub 2011 Nov 29. PMID: 22128302. |
| In vivo protocol: | 1. Fu YY, Cen JK, Song HL, Song SY, Zhang ZJ, Lu HJ. Ginsenoside Rh2 Ameliorates Neuropathic Pain by inhibition of the miRNA21-TLR8-mitogen-activated protein kinase axis. Mol Pain. 2022 Apr;18:17448069221126078. doi: 10.1177/17448069221126078. PMID: 36039405; PMCID: PMC9478689. 2. Zhao LX, Jiang M, Bai XQ, Cao DL, Wu XB, Zhang J, Guo JS, Chen TT, Wang J, Wu H, Gao YJ, Zhang ZJ. TLR8 in the Trigeminal Ganglion Contributes to the Maintenance of Trigeminal Neuropathic Pain in Mice. Neurosci Bull. 2021 Apr;37(4):550-562. doi: 10.1007/s12264-020-00621-4. Epub 2020 Dec 23. PMID: 33355900; PMCID: PMC8055805. |
1: Lu H, Dietsch GN, Matthews MA, Yang Y, Ghanekar S, Inokuma M, Suni M, Maino VC, Henderson KE, Howbert JJ, Disis ML, Hershberg RM. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509. doi: 10.1158/1078-0432.CCR-11-1625. Epub 2011 Nov 29. PubMed PMID: 22128302.
