TMP778

This product is for research use only, not for human use. We do not sell to patients.

TMP778
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
100mg$3225To Be Confirmed
200mg$4835To Be Confirmed
500mg$8160To Be Confirmed

Cat #: V7133 CAS #: 1422053-04-0 Purity ≥ 99%

Description: TMP778 (TMP-778; TMP 778) is a novel and potent RORγt inverse agonist with potential anti-inflammatory activity.

References: Skepner J, et al. Pharmacologic inhibition of RORγt regulates Th17 signature gene expression and suppresses cutaneous inflammation in vivo. J Immunol. 2014 Mar 15;192(6):2564-75.

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Molecular Weight (MW)494.58
Molecular FormulaC31H30N2O4
CAS No.1422053-04-0
SMILES CodeCC1=NOC(C)=C1[C@H](O)C2=CC3=CC(CC(N[C@@H](C4=CC=CC=C4)C5=CC=C(C=C5C)C)=O)=CC=C3O2
SynonymsTMP778; TMP-778; TMP 778
ProtocolIn VitroIt is found that TMP778 at >2.5 μM starts to show toxic effects on cell growth, which however is not RORγt-dependent, since the proliferation of RORγt-deficient T cells cultured under Th17 cell-polarizing conditions is also decreased. Otherwise, these inhibitors do not show inhibitory effects on cell proliferation or RORγt expression or its nuclear translocation, but efficiently inhibited IL-17 production. TMP778 has a much broader dose range and efficiently decreased IL-17 production, consistent with its higher binding affinity for RORγt. These data indicate that TMP778 is the RORγt inhibitor that most potently reduced IL-17 production.
In VivoAll three compounds (e.g., TMP778) delay the onset of disease and substantially reduce the severity of disease progression compared to control-treated mice. Consistent with in vitro results, TMP778 treatment causes the most pronounced effect on the disease phenotype. This treatment not only decreases the number of mononuclear cells infiltrating the central nervous system (CNS), but also most strongly reduces the percentage of IL-17+ T cells in the CNS (including IL-17+ IFNγ+). There is no significant change in the percentage IFNγ+ IL-17-T cells in the CNS among all groups, indicating that none of the inhibitors affects Th1 responses. TMP778 strongly inhibits Th17 cell generation, reduces IL-17 production from differentiated Th17 cells, and also dramatically ameliorates the progression of EAE.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.0219 mL10.1096 mL20.2192 mL40.4384 mL
5mM0.4044 mL2.0219 mL4.0438 mL8.0877 mL
10mM0.2022 mL1.0110 mL2.0219 mL4.0438 mL
20mM0.1011 mL0.5055 mL1.0110 mL2.0219 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

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Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.