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| 25mg |
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| Targets |
MHV-370 targets Toll-like receptors 7 and 8 (TLR7/8). TLR7 and TLR8 are pattern recognition receptors that recognize single-stranded RNA and are involved in the innate immune response. By potently and selectively inhibiting these receptors, MHV-370 blocks the downstream signaling cascade that leads to the production of type I interferons and other pro-inflammatory cytokines.
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| ln Vitro |
TLR7/8-IN-1 is an inhibitor of TLR7/TLR8 that is crystalline. Autoimmune illness research can benefit from the usage of TLR7/8-IN-1 [1].
In vitro, MHV-370 demonstrates potent inhibition of TLR7 and TLR8 with IC50 values of 1.1 nM and 4.5 nM in cell-based assays. As a dual TLR7/8 inhibitor, it effectively blocks the activation of these receptors and the subsequent production of inflammatory mediators. Its high potency and selectivity make it a valuable tool for studying TLR7/8-driven inflammation. |
| ln Vivo |
In vivo data for MHV-370 is not extensively reported in publicly available sources. As a potent, selective, and orally bioavailable TLR7/8 inhibitor, the compound has potential applications in animal models of autoimmune and inflammatory diseases. By suppressing aberrant innate immune activation, MHV-370 could provide therapeutic benefits in conditions such as lupus and psoriasis. However, specific published in vivo efficacy studies are not detailed in the current literature.
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| Enzyme Assay |
The in vitro TLR7/8 inhibition assay for MHV-370 typically uses cell lines expressing human TLR7 or TLR8 and a reporter gene under the control of an NF-κB-responsive element. Cells are stimulated with a TLR7/8 agonist in the presence of varying concentrations of MHV-370. The inhibition of TLR7/8 activation is measured by quantifying the reporter gene activity. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for MHV-370 are conducted in immune cells such as peripheral blood mononuclear cells (PBMCs) or specific TLR7/8-expressing cell lines. Cells are treated with varying concentrations of MHV-370 and stimulated with TLR7/8 agonists. The production of cytokines such as TNF-α, IL-6, and type I interferons is measured by ELISA or qPCR. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo studies for MHV-370 would typically involve mouse models of autoimmune or inflammatory diseases where TLR7/8 signaling is implicated. The compound would be administered orally. Efficacy would be assessed by measuring disease severity, inflammatory cytokine levels, and immune cell activation. However, specific published in vivo protocols for MHV-370 are not available in the current literature.
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| ADME/Pharmacokinetics |
MHV-370 is an orally bioavailable compound. It has a molecular formula of C29H40N8O2 and a molecular weight of 532.68. As a small molecule TLR7/8 inhibitor, it is expected to have good oral absorption. Detailed PK parameters such as half-life and bioavailability are not extensively reported in the provided sources.
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| Toxicity/Toxicokinetics |
Toxicity data for MHV-370 is limited. As with all research compounds, MHV-370 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
MHV-370 (MHV370; CAS 2205095-75-4) is a potent, selective, and orally bioavailable dual inhibitor of TLR7/8 with IC50 values of 1.1 nM and 4.5 nM. It is designed to suppress aberrant innate immune activation and pathological type I interferon signaling. MHV-370 is used in research on autoimmune and inflammatory diseases. It is for research use only.
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| Molecular Formula |
C29H40N8O2
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|---|---|
| Molecular Weight |
532.68
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| Exact Mass |
532.327
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| CAS # |
2205095-75-4
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| PubChem CID |
134330557
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| Appearance |
White to off-white solid powder
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| LogP |
1.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
39
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| Complexity |
895
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(N1N=C(C)C2CN(C3C=C(C)N=C4N(C)N=CC=34)CCC1=2)C12CCC(NC([C@H]3NCCOC3)=O)(CC1)CC2
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| InChi Key |
OXDQXRVWDYGAHX-SAVAPUMLSA-N
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| InChi Code |
InChI=1S/C29H40N8O2/c1-19-14-25(21-15-31-35(3)26(21)32-19)36-12-4-24-22(16-36)20(2)34-37(24)18-28-5-8-29(9-6-28,10-7-28)33-27(38)23-17-39-13-11-30-23/h14-15,23,30H,4-13,16-18H2,1-3H3,(H,33,38)/t23-,28?,29?/m0/s1
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| Chemical Name |
(3S)-N-[4-[[5-(1,6-dimethylpyrazolo[3,4-b]pyridin-4-yl)-3-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-1-yl]methyl]-1-bicyclo[2.2.2]octanyl]morpholine-3-carboxamide
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| Synonyms |
MHV370; MHV-370
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~23.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8773 mL | 9.3865 mL | 18.7730 mL | |
| 5 mM | 0.3755 mL | 1.8773 mL | 3.7546 mL | |
| 10 mM | 0.1877 mL | 0.9386 mL | 1.8773 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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