[CAS NO. 1221186-53-3] TEPP-46

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PRODUCTS SPECIFICATIONS [1221186-53-3]

Catalog

HY-18657

Brand

MCE

CAS

1221186-53-3

DESCRIPTION [1221186-53-3]

Overview

MDL	-
Molecular Weight	372.46
Molecular Formula	C17H16N4O2S2
SMILES	O=C1C(N(C)C2=C3SC(S(C)=O)=C2)=C3C=NN1CC4=CC=CC(N)=C4

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

20 Publications Citing Use of MCE

Summary

TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC ₅₀ of 92 nM, showing little or no effect on PKM1, PKL and PKR ^[1] .

In Vitro

TEPP-46 and DASA-58 activate PKM2 by a mechanism similar to that of the endogenous activator FBP. Pre-treatment of cells with TEPP-46 or DASA-58 prevents pervanadate-induced inhibition of PKM2 activity. TEPP-46 also induces a decrease in the intracellular levels of acetyl-coA, lactate, ribose phosphate and serine ^[1] . TEPP-46 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes. TEPP-46 treatment significantly downregulates the expression of the M1 markers Il12p40 and Cxcl-10. Activation of PKM2 using TEPP-46 significantly inhibits FSL-1 and CpG-induced Il1b mRNA expression. TEPP-46 inhibits Mtb-induced Il1b mRNA levels, boosts Mtb-induced levels of Il10 mRNA, and has no effect on levels of Tnf ^[2] .

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

In Vivo

TEPP-46 exhibits good oral bioavailability with relatively low clearance, long half-life, and good volume of distribution-parameters that predict for drug exposure in tumor tissues. TEPP-46 at 150 mg/kg readily achieves maximal PKM2 activation measured in A549 xenograft tumors ^[1] .

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

Appearance

Solid

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 : 50 mg/mL ( 134.24 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6849 mL	13.4243 mL	26.8485 mL
5 mM	0.5370 mL	2.6849 mL	5.3697 mL
10 mM	0.2685 mL	1.3424 mL	2.6849 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 50% PEG300 >> 50% saline

Solubility: 10 mg/mL (26.85 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.87 mg/mL (7.71 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (6.71 mM); Suspended solution; Need ultrasonic
5.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

5H-Thieno[2′,3′:4,5]pyrrolo[2,3-d]pyridazin-5-one, 6-[(3-aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-

6-[(3-Aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2′,3′:4,5]pyrrolo[2,3-d]pyridazin-5-one

TEPP-46