2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. TMP778

TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.

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

TMP778 Chemical Structure

TMP778 Chemical Structure

CAS No. : 1422053-04-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 490 In-stock
Solution
10 mM * 1 mL in DMSO USD 490 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2550 In-stock
100 mg USD 3800 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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TMP778 Related Antibodies

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Description

TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.

IC50 & Target

IC50: 7 nM (FRET assay), 63 nM (IL-17F promoter assay), 0.03 μM (in Th17 cells), 0.005 μM (in Tc17 cells)[1].
Cellular Effect
Cell Line Type Value Description References
Jurkat IC50
63 nM
Compound: 8; TMP778
Inverse agonist activity at RORgamma (unknown origin) expressed in human Jurkat cells assessed as inhibition of IL-17F production after 20 hrs by luciferase reporter gene assay
Inverse agonist activity at RORgamma (unknown origin) expressed in human Jurkat cells assessed as inhibition of IL-17F production after 20 hrs by luciferase reporter gene assay
[PMID: 27542308]
In Vitro

It 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[2].

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

TMP778 Related Antibodies
In Vivo

All 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[2].

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

494.58

Formula

C31H30N2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=NOC(C)=C1[C@@H](C2=CC3=CC(CC(N[C@H](C4=CC=C(C)C=C4C)C5=CC=CC=C5)=O)=CC=C3O2)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 : 240 mg/mL (485.26 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 2.0219 mL 10.1096 mL 20.2192 mL
5 mM 0.4044 mL 2.0219 mL 4.0438 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Cell Assay
[2]

Naive CD4+ T cells are activated in 96-well plates under Th17 cell polarizing conditions in the presence of indicated doses of RORγt inhibitors (e.g., TMP778: 30, 10, 2.5, 0.83, 0.28, 0.09 μM ) or vehicle control DMSO. After 48 h, plates are pulsed for 16 h with 1 μCi 3H-thymidine per well. Proliferation is measured as counts per minute by using a Wallac Liquid Scintillation Counter[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
EAE is induced in C57BL/6 mice with MOG35-55 plus CFA immunization in conjunction with subcutaneous administration of the inhibitors twice daily from day 0. C57BL/6 mice are immunized with MOG35-55 plus CFA, and RORγt inhibitor (TMP778, 200 μg per injection, n=19; TMP920, 500 μg per injection, n=7; Digoxin, 50 μg per injection, n=5, >100 μg cause mouse death; DMSO, n=19) are subcutaneously injected twice daily starting from day 0. Mice are evaluated daily for signs of EAE. When 11 days after groups of mice treated with different RORγt inhibitors are compared with the group of mice with DMSO (vehicle control) treatment[2].

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

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0219 mL 10.1096 mL 20.2192 mL 50.5479 mL
5 mM 0.4044 mL 2.0219 mL 4.0438 mL 10.1096 mL
10 mM 0.2022 mL 1.0110 mL 2.0219 mL 5.0548 mL
15 mM 0.1348 mL 0.6740 mL 1.3479 mL 3.3699 mL
20 mM 0.1011 mL 0.5055 mL 1.0110 mL 2.5274 mL
25 mM 0.0809 mL 0.4044 mL 0.8088 mL 2.0219 mL
30 mM 0.0674 mL 0.3370 mL 0.6740 mL 1.6849 mL
40 mM 0.0505 mL 0.2527 mL 0.5055 mL 1.2637 mL
50 mM 0.0404 mL 0.2022 mL 0.4044 mL 1.0110 mL
60 mM 0.0337 mL 0.1685 mL 0.3370 mL 0.8425 mL
80 mM 0.0253 mL 0.1264 mL 0.2527 mL 0.6318 mL
100 mM 0.0202 mL 0.1011 mL 0.2022 mL 0.5055 mL
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TMP778 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:

TMP7781422053-04-0TMP 778TMP-778RORRAR-related orphan receptorInhibitorinhibitorinhibit

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