1. L-733060 hydrochloride

L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent.

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L-733060 hydrochloride Chemical Structure

L-733060 hydrochloride Chemical Structure

CAS No. : 148687-76-7

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Description

L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent[1][2].

IC50 & Target

NK1 Receptor[1]

In Vitro

L-733060 (30-300 nM) inhibits the [Ca2+]i mobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK1 receptor-transfected CHO cells[1].
L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells[2].
L-733060 (10-30 μM; 24 and 48 h) inhibits MEL H0 cells proliferation with IC50s of 27.5 μM and 18.9 μM at 24 h and 48 h, respectively[2].
L-733060 (20-50 μM; and or 72 h) inhibits COLO 679 cells growth with IC50s of 33.8 μM and 31.5 μM at 30 h and 72 h, respectively[2].

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

Cell Proliferation Assay[2]

Cell Line: COLO 858 cells
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 0, 48, 96 h
Result: Inhibited cells growth with IC50s of 8.7 μM and 7.1 μM at 48 h and 96 h, respectively.
In Vivo

L-733060 (10-1000 μg/kg; i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats[1].
L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000 μg/kg in conscious or anaesthetised rats[1].

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

Animal Model: Male Sprague-Dawley rats (200 g) with electrical stimulation of the trigeminal ganglion[1]
Dosage: 10, 100, 1000 mg/kg
Administration: I.v. injection
Result: Produced a significant dose-related inhibition of plasma extravasation with an ID50 of 212±19 μg/kg.
Molecular Weight

439.82

Formula

C20H20ClF6NO

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(C1=CC(C(F)(F)F)=CC(CO[C@@H]2[C@@](C3=CC=CC=C3)([H])NCCC2)=C1)F.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°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: 

H2O : 22 mg/mL (50.02 mM; Need warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2737 mL 11.3683 mL 22.7366 mL
5 mM 0.4547 mL 2.2737 mL 4.5473 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

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 (sealed storage, away from moisture). 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
H2O 1 mM 2.2737 mL 11.3683 mL 22.7366 mL 56.8414 mL
5 mM 0.4547 mL 2.2737 mL 4.5473 mL 11.3683 mL
10 mM 0.2274 mL 1.1368 mL 2.2737 mL 5.6841 mL
15 mM 0.1516 mL 0.7579 mL 1.5158 mL 3.7894 mL
20 mM 0.1137 mL 0.5684 mL 1.1368 mL 2.8421 mL
25 mM 0.0909 mL 0.4547 mL 0.9095 mL 2.2737 mL
30 mM 0.0758 mL 0.3789 mL 0.7579 mL 1.8947 mL
40 mM 0.0568 mL 0.2842 mL 0.5684 mL 1.4210 mL
50 mM 0.0455 mL 0.2274 mL 0.4547 mL 1.1368 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Product Name:
L-733060 hydrochloride
Cat. No.:
HY-14406A
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