Pentoxyverine (Synonyms: Carbetapentane)

Name: Pentoxyverine
Brand: MedChemExpress
SKU: HY-134004
Rating: 4.5 (0 reviews)

Cat. No.: HY-134004 Purity: 99.56%: Data Sheet
COA

SDS
Handling Instructions
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Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.

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Pentoxyverine 화학구조

CAS No. : 77-23-6

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

Other Forms of Pentoxyverine:

Pentoxyverine citrate In-stock
Pentoxyverine (Standard) 견적 받기

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•Related Screening Libraries:

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View All Sigma Receptor Isoform Specific Products:

View All Isoforms

Sigma 1 Receptor Sigma 2 Receptor

View All mAChR Isoform Specific Products:

View All Isoforms

mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

σ1

41 nM (Ki)

σ2

894 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
Astrocyte	EC₅₀	28.16 3 Compound: 10	Antiproliferative activity against mouse astrocyte cells by MTT assay Antiproliferative activity against mouse astrocyte cells by MTT assay	[PMID: 17417631]
Astrocyte	EC₅₀	28.16 3 Compound: 10	Antiproliferative activity against mouse astrocyte cells by MTT assay Antiproliferative activity against mouse astrocyte cells by MTT assay	[PMID: 17417631]
Astrocyte	EC₅₀	28.16 3 Compound: 10	Antiproliferative activity against mouse astrocyte cells by MTT assay Antiproliferative activity against mouse astrocyte cells by MTT assay	[PMID: 17417631]
HEK293	IC₅₀	1.55 3 Compound: Carbetapentane	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay	[PMID: 28230985]
HEK293	IC₅₀	1.55 3 Compound: Carbetapentane	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay	[PMID: 28230985]
HEK293	IC₅₀	1.55 3 Compound: Carbetapentane	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay	[PMID: 28230985]
Medulloblastoma cell	EC₅₀	2.083 3 Compound: 10	Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay	[PMID: 17417631]
Medulloblastoma cell	EC₅₀	2.083 3 Compound: 10	Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay	[PMID: 17417631]
Medulloblastoma cell	EC₅₀	2.083 3 Compound: 10	Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay	[PMID: 17417631]

In Vivo

Pentoxyverine (Carbetapentane; 1-32 mg/kg; SC) dose-dependently potentiates the sensitizing effect of capsaicin to the mechanical stimulus when the mice were stimulated in the paw injected with Capsaicin (HY-10448)^[4].
Pentoxyverine (16 mg/kg; SC) shows strong potentiation of Capsaicin-induced secondary mechanical allodynia^[4].
Pentoxyverine (50 mg/kg; orally; ), used for positive control, increases the percentage of the aqueous ammonia-induced latent period of cough by 121.72%, inhibits cough frequency by 45.45% after administration for 7 days in mice of either sex (22-25 g)^[5].

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

Animal Model:	Female wild-type weighing 25 to 30 g^[4]
Dosage:	0.5, 1, 2, 4, 8, 16, 32 mg/kg
Administration:	SC; 30 min before the intraplantar (i.pl.) administration of capsaicin (0.125 μg)
Result:	Dose-dependently potentiated the sensitizing effect of capsaicin to the mechanical stimulus when the mice were stimulated in the paw injected with capsaicin.

분자량

333.47

화학식

C₂₀H₃₁NO₃

CAS No.

77-23-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1(C2=CC=CC=C2)CCCC1)OCCOCCN(CC)CC

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 250 mg/mL (749.69 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	2.9988 mL	14.9939 mL	29.9877 mL
5 mM	0.5998 mL	2.9988 mL	5.9975 mL
10 mM	0.2999 mL	1.4994 mL	2.9988 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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.56%

Select Batch:

Data Sheet (274 KB) SDS (254 KB)

COA (247 KB) HNMR (271 KB) RP-HPLC (226 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Calderon SN, et, al. Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands. J Med Chem. 1994 Jul 22;37(15):2285-91. [Content Brief]

[2]. Brown C, et, al. Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004 Jan;141(2):233-40. [Content Brief]

[3]. Mohamed SH, et, al. Extraction-free spectrophotometric assay of the antitussive drug pentoxyverine citrate using sulfonephthalein dyes. Spectrochim Acta A Mol Biomol Spectrosc. 2019 Nov 5;222:117186. [Content Brief]

[4]. J M Entrena, et al. Sigma-1 Receptor Agonism Promotes Mechanical Allodynia After Priming the Nociceptive System with Capsaicin. Sci Rep. 2016 Nov 25:6:37835. doi: 10.1038/srep37835. [Content Brief]

[5]. Yuebin Ge, et al. In Vivo Evaluation of the Antiasthmatic, Antitussive, and Expectorant Activities and Chemical Components of Three Elaeagnus Leaves. Evid Based Complement Alternat Med. 2015:2015:428208. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9988 mL	14.9939 mL	29.9877 mL	74.9693 mL
	5 mM	0.5998 mL	2.9988 mL	5.9975 mL	14.9939 mL
	10 mM	0.2999 mL	1.4994 mL	2.9988 mL	7.4969 mL
	15 mM	0.1999 mL	0.9996 mL	1.9992 mL	4.9980 mL
	20 mM	0.1499 mL	0.7497 mL	1.4994 mL	3.7485 mL
	25 mM	0.1200 mL	0.5998 mL	1.1995 mL	2.9988 mL
	30 mM	0.1000 mL	0.4998 mL	0.9996 mL	2.4990 mL
	40 mM	0.0750 mL	0.3748 mL	0.7497 mL	1.8742 mL
	50 mM	0.0600 mL	0.2999 mL	0.5998 mL	1.4994 mL
	60 mM	0.0500 mL	0.2499 mL	0.4998 mL	1.2495 mL
	80 mM	0.0375 mL	0.1874 mL	0.3748 mL	0.9371 mL
	100 mM	0.0300 mL	0.1499 mL	0.2999 mL	0.7497 mL

Pentoxyverine Related Classifications

Neurological Disease Inflammation/Immunology

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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Pentoxyverine (Synonyms: Carbetapentane)

고객리뷰

Other Forms of Pentoxyverine:

Pentoxyverine Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sigma Receptor Isoform Specific Products:

View All mAChR Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Pentoxyverine Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report