Doxylamine succinate

Name: Doxylamine succinate
Brand: MedChemExpress
SKU: HY-A0069
Rating: 4.5 (1 reviews)

Cat. No.: HY-A0069 Purity: 99.44%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia.

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

Doxylamine succinate Chemical Structure

CAS No. : 562-10-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	Get quote
50 g	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Doxylamine succinate:

Doxylamine-d₅ succinate Get quote
Doxylamine Get quote
Doxylamine succinate (Standard) Get quote

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•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

H₁ Receptor

Parmacokinetics

Species	Dose	Route	AUC_0-12	C_max	T_max	Bioavailability
Rat^[3]	1 ug	i.n.	3339.2 ng·h/mL	887.6 ng/mL	0.5 h	70.8 %
Rat^[3]	2000 ug	p.o.	1163.2 ng·h/mL	281.4 ng/mL	1.5 h	24.7 %
Rat^[3]	0.001 μg	i.v.	4715.0 ng·h/mL	1296.4 ng/mL	/	/

In Vivo

Doxylamine succinate (administered daily via diet for 7 or 15 days at doses of 40-1500 ppm) acts as a phenobarbital-type inducer of hepatic microsomal cytochrome P450 in B6C3F1 mice, with a maximum 38-fold induction of CYP2B activity; at the highest dose, it also alters thyroid hormone homeostasis by decreasing serum T₄ and increasing serum TSH^[1].
Doxylamine succinate (1-2 mg; 4% solution (25 μL); oral administration; intravenous injection; intranasal administration; single dose) shows a bioavailability of 70.8% via intranasal delivery in male Sprague-Dawley rats, with rapid absorption and no nasal epithelial damage^[3].

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

Animal Model:	B6C3F1/CrlBR VAF/Plus (male and female, 45-52 days old)^[1]
Dosage:	40, 375, 750, 1500 ppm (dietary, free base equivalent); 10, 86, 173, 349 mg/kg/day (male) (7 days); 9, 84, 166, 395 mg/kg/day (male) (15 days); 10, 102, 198, 416 mg/kg/day (female) (7 days); 12, 104, 204, 446 mg/kg/day (female) (15 days)
Administration:	dietary; daily; 7 or 15 days
Result:	Elevated liver weight significantly in a dose-related manner at ≥ 375 ppm in both sexes following 7‑day and 15‑day treatments. Induced hepatic microsomal cytochrome P450 and overall hepatic metabolic activity dose‑dependently in all treated animals, strongly upregulating the functions of CYP2B, CYP3A and CYP2A subfamilies. Increased thyroxine‑glucuronosyltransferase activity with obvious sex and dose differences, and raised adjusted total hepatic activity. Disrupted thyroid endocrine homeostasis by elevating serum TSH, lowering serum T4 universally, and causing only slight T3 reduction in high‑dose females.

Clinical Trial

Molecular Weight

388.46

Formula

C₂₁H₂₈N₂O₅

CAS No.

562-10-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CCC(O)=O.CC(C1=NC=CC=C1)(C2=CC=CC=C2)OCCN(C)C

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:

DMSO : ≥ 100 mg/mL (257.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (128.71 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5743 mL	12.8713 mL	25.7427 mL
5 mM	0.5149 mL	2.5743 mL	5.1485 mL
10 mM	0.2574 mL	1.2871 mL	2.5743 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

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: ≥ 2.5 mg/mL (6.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (257.43 mM); Clear solution; Need ultrasonic

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.

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

Purity: 99.76%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (245 KB) HNMR (143 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[1]. Bookstaff RC, et al. Effects of doxylamine succinate on thyroid hormone balance and enzyme induction in mice. Toxicol Appl Pharmacol. 1996;141(2):584-594.

[2]. Nuangchamnong N, et al. Doxylamine succinate-pyridoxine hydrochloride (Diclegis) for the management of nausea and vomiting in pregnancy: an overview. Int J Womens Health. 2014;6:401-409.

[3]. Pelser A, et al. Comparative pharmacokinetics of single doses of doxylamine succinate following intranasal, oral and intravenous administration in rats. Biopharm Drug Dispos. 2002;23(6):239-244.

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.5743 mL	12.8713 mL	25.7427 mL	64.3567 mL
	5 mM	0.5149 mL	2.5743 mL	5.1485 mL	12.8713 mL
	10 mM	0.2574 mL	1.2871 mL	2.5743 mL	6.4357 mL
	15 mM	0.1716 mL	0.8581 mL	1.7162 mL	4.2904 mL
	20 mM	0.1287 mL	0.6436 mL	1.2871 mL	3.2178 mL
	25 mM	0.1030 mL	0.5149 mL	1.0297 mL	2.5743 mL
	30 mM	0.0858 mL	0.4290 mL	0.8581 mL	2.1452 mL
	40 mM	0.0644 mL	0.3218 mL	0.6436 mL	1.6089 mL
	50 mM	0.0515 mL	0.2574 mL	0.5149 mL	1.2871 mL
	60 mM	0.0429 mL	0.2145 mL	0.4290 mL	1.0726 mL
	80 mM	0.0322 mL	0.1609 mL	0.3218 mL	0.8045 mL
	100 mM	0.0257 mL	0.1287 mL	0.2574 mL	0.6436 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.