1. Metabolic Enzyme/Protease
  2. Nampt
  3. Teglarinad chloride

Teglarinad chloride (Synonyms: GMX1777; EB-1627)

Cat. No.: HY-10080 Purity: 98.07%
Handling Instructions

Teglarinad chloride (GMX1777) is a prodrug of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis.

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

Teglarinad chloride Chemical Structure

Teglarinad chloride Chemical Structure

CAS No. : 432037-57-5

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5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
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25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
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100 mg USD 3400 In-stock
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Description

Teglarinad chloride (GMX1777) is a prodrug of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis[1][2].

In Vivo

GMX1777 (75 mg/kg; 24 h intravenous infusion) causes tumor regression in the IM-9 model, a small-cell lung cancer (SHP-77) model, and a colon carcinoma (HCT-116) model[2].
GMX1777 (50-100 mg/kg/d, i.m. for 5 d) with or without local tumor radiotherapy is effective for both FaDu and C666-1 tumors in vivo[1].
GMX1777 (25-400 mg/kg; 24 h intravenous infusion) is quickly converted to GMX1778 in plasma of mice with a half-life of GMX1777 less than 0.7 h[2].

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

Animal Model: CB17 SCID/SCID female mice bearing subcutaneous IM-9 multiple myeloma tumors[2]
Dosage: 18.75, 35, 75 mg/kg
Administration: A 24 h intravenous infusion
Result: Induced a nearly complete regression of the tumors and a significant tumor growth delay at the dose of 75 mg/kg.
Reduced IM-9 tumor growth moderately at 37.5 mg/kg.
Molecular Weight

672.60

Formula

C₃₀H₄₃Cl₂N₅O₈

CAS No.

432037-57-5

SMILES

N#CN/C(NC1=CC=[N+](C=C1)COC(OCCOCCOCCOCCOC)=O)=N/CCCCCCOC2=CC=C(C=C2)Cl.[Cl-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (297.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4868 mL 7.4338 mL 14.8677 mL
5 mM 0.2974 mL 1.4868 mL 2.9735 mL
10 mM 0.1487 mL 0.7434 mL 1.4868 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 5 mg/mL (7.43 mM); Clear solution

  • 2.

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

    Solubility: ≥ 5 mg/mL (7.43 mM); Clear solution

  • 3.

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

    Solubility: ≥ 5 mg/mL (7.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TeglarinadGMX1777 EB-1627GMX 1777GMX-1777EB1627EB 1627EB-1627NamptNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorGMX1778nicotinamidephosphoribosyltransferase,NAMPTradiationDNArepairantiangiogenesisantitumorInhibitorinhibitorinhibit

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Product Name:
Teglarinad chloride
Cat. No.:
HY-10080
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