TMP778
Based on 1 Customer Validation
TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.98%
- CAS. Nr.: 1422053-04-0
- Formel: C31H30N2O4
- Molecular Weight:494.58
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-13421
SR1001RORα/γt Inverse Agonist -
HY-14422
SR1078RORα/RORγ Agonist -
HY-19775
GNE-6468RORγ (RORc) Inverse Agonist -
HY-14413
SR3335RORα Inverse Agonist -
HY-101454
SR0987RORγt Agonist -
HY-104037
CintirorgonRORγ Agonist -
HY-112706
PF-06747711RORγt Inverse Agonist -
HY-19770
GSK2981278RORγ Inverse Agonist -
HY-119366
S18-000003RORγt Inhibitor -
HY-13421R
SR1001 (Standard)RORα/γt Inverse Agonist -
HY-12776
GSK805RORγt Inhibitor -
HY-102075AR
TMP778 (Standard)Reference Standard
Biologische Aktivität
Beschreibung
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
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Cell Line
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Type | Value | Description | References |
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| Jurkat | IC50 |
63 nM
Compound: 8; TMP778
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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
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[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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1422053-04-0
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Appearance Solid
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Molecular Weight 494.58
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Formel C31H30N2O4
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Color White to off-white
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. 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. [Content Brief]
[2]. Xiao S, et al. Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms. Immunity. 2014 Apr 17;40(4):477-89. [Content Brief]
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 |
TMP778 Related Classifications
HY-102075A Related Classifications
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