Art. -Nr.: HY-B0383

Almotriptan malate

(Synonyms: PNU180638)

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Based on 1 Customer Validation

Almotriptan malate (PNU180638) is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.

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Reinheit: 99.53%
CAS. Nr.: 181183-52-8
Formel: C₂₁H₃₁N₃O₇S
Molecular Weight:469.55

Speicherung:

4°C, sealed storage, away from moisture

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

Almotriptan malate Chemical Structure

CAS. Nr.: 181183-52-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]

5-HT_1B Receptor

1.6 nM (EC₅₀)

5-HT_1D Receptor

3.1 nM (EC₅₀)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Almotriptan malate acts as a full agonist to induce potent concentration-dependent contractions in canine isolated saphenous veins, with an EC₅₀ of 394 nM, via 5-HT₁B/1D receptors^[2].
Almotriptan malate induces vasoconstriction in human isolated meningeal, superficial temporal, and basilar arteries, with EC₅₀ values of 0.7 μM (superficial temporal) and 3.7 μM (basilar), and greater potency than Sumatriptan (HY-B0121B) in meningeal arteries^[2].
Almotriptan malate is metabolized by multiple human liver microsomal enzymes, including MAO-A, FMO, aldehyde dehydrogenase, CYP2D6, and CYP3A4, and only weakly inhibits CYP2D6 with no significant inhibition of MAO-A or MAO-B^[2].

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

Parmacokinetics

Species	Dose	Route	Note	T_max	C_max	AUC	T_1/2	V_z	CL	F
Rat^[2]	10 mg/kg	i.v.	male	0.1 h	3.43 μg/mL	1.69 μg·h/mL	0.8 h	6.4 L/kg	5.9 L/h/kg	/
Rat^[2]	10 mg/kg	i.v.	female	0.1 h	3.60 μg/mL	1.82 μg·h/mL	0.7 h	5.3 L/kg	5.5 L/h/kg	/
Rat^[2]	10 mg/kg	s.c.	male	0.5 h	1.55 μg/mL	1.75 μg·h/mL	0.6 h	4.9 L/kg	5.7 L/h/kg	104 %
Rat^[2]	10 mg/kg	s.c.	female	0.5 h	1.58 μg/mL	1.99 μg·h/mL	0.8 h	5.5 L/kg	5.0 L/h/kg	109 %
Rat^[2]	10 mg/kg	p.o.	male	0.25 h	0.57 μg/mL	0.62 μg·h/mL	2.0 h	/	/	37 %
Rat^[2]	10 mg/kg	p.o.	female	0.25 h	0.45 μg/mL	0.64 μg·h/mL	1.2 h	/	/	35 %
Dog^[2]	5 mg/kg	i.v.	/	0.1 h	1.95 μg/mL	4.39 μg·h/mL	2.3 h	3.7 L/kg	1.2 L/h/kg	/
Dog^[2]	5 mg/kg	s.c.	/	0.5 h	1.6 μg/mL	5.14 μg·h/mL	2.8 h	/	/	118 %
Dog^[2]	5 mg/kg	p.o.	/	0.8 h	0.92 μg/mL	3.60 μg·h/mL	2.4 h	/	/	82 %
Cynomolgus Monkey^[2]	10 mg/kg	i.v.	/	0.08 h	5.18 μg/mL	4.32 μg·h/mL	1.3 h	4.4 L/kg	2.4 L/h/kg	/
Cynomolgus Monkey^[2]	10 mg/kg	p.o.	/	3.5 h	0.20 μg/mL	0.79 μg·h/mL	1.7 h	/	/	19 %

In Vivo

Almotriptan (0.01-3000 μg/kg; intravenous/intradermal administration; single dose) malate increases carotid vascular resistance in anesthetized cats, with efficacy and potency comparable to those of Sumatriptan; it elevates resistance by 100% at an intravenous dose of 9 μg/kg and exerts effects via the 5-HT₁ receptor^[2].
Almotriptan (0-1 mg/kg; intravenous injection; single dose; maximum 0.3 mg/kg; intravenous injection; single dose; 30 μg/min; intracoronary infusion; 1 h) malate increases carotid vascular resistance in beagle dogs, and exhibits better carotid-femoral artery selectivity than Sumatriptan. At the tested doses, this agent has favorable cardiovascular safety, with no cardiac inhibitory effect or QTc interval change^[2].
Almotriptan (10 mg/kg; subcutaneous injection; single dose) malate inhibits trigeminal ganglion-induced meningeal vascular extravasation in anesthetized guinea pigs, and at a subcutaneous dose of 10 mg/kg, it causes no hypothermia or bronchospasm in conscious guinea pigs^[2].
Almotriptan (oral administration; single dose) malate does not alter cardiovascular parameters or diuretic effects in normotensive Wistar rats at the tested oral doses^[2].
Almotriptan (1-3 mg/kg; subcutaneous injection; single administration) malate exerts no cardiovascular effects at the dose of 1 mg/kg s.c. in conscious cynomolgus monkeys, while the 3 mg/kg s.c. dose only induces mild, transient effects without electrocardiogram changes^[2].
Almotriptan (up to 300 mg/kg; p.o.; single administration) malate shows no central nervous system-related behavioral or motor function effects in mice at oral doses up to 300 mg/kg^[2].
Almotriptan malate slightly alleviates apomorphine (HY-12723)-induced vomiting responses in dogs^[2].

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

Animal Model:

Domestic cat (anesthetized)^[2]
Dosage:

9 μg/kg (i.v.); 0.01-3000 μg/kg (i.v.); unspecified (i.d.)
Administration:

i.v.; single dose; i.d.; single dose
Result:

Increased carotid vascular resistance by 100%.
Produced statistically significant increases in carotid vascular resistance at doses ≥10 μg/kg i.v..
Showed effective enteric absorption via i.d.
administration, increasing carotid vascular resistance with potency and efficacy equivalent to sumatriptan.
Acted mainly on carotid arteriovenous anastomoses, had a tendency to increase cerebral blood flow in absolute and relative terms, and did not decrease the component of brain blood flow supplied by the carotid artery.
Carotid vasoconstrictor effects were almost completely reversed by methiothepin, a 5-HT₁ receptor antagonist.

Animal Model:

Beagle dog (anesthetized, conscious)^[2]
Dosage:

unspecified (carotid effect); 1 mg/kg; up to 0.3 mg/kg; 30 μg/min
Administration:

i.v.; single dose; intracoronary infusion; 1 hour
Result:

Increased carotid vascular resistance and showed greater selectivity for carotid versus femoral vascular beds compared to sumatriptan.
At 1 mg/kg i.v., produced a moderate increase in renal blood flow and a transient increase in diuresis and natriuresis, with no effect on glomerular filtration rate or filtration fraction.
At doses up to 0.3 mg/kg i.v.
in conscious dogs, had no effect on coronary blood flow or coronary vascular resistance, and produced no changes in evaluated ECG intervals.
Intracoronary infusion at 30 μg/min for 1 hour did not alter the QTc interval.
Did not induce a cardiodepressant effect (fall in heart rate and dP/dt_max) in open-chest anesthetized dogs, unlike sumatriptan.

Animal Model:

Guinea pig (anesthetized, conscious)^[2]
Dosage:

10 mg/kg
Administration:

s.c.; single dose
Result:

Inhibited meningeal extravasation produced by electrical stimulation of the trigeminal ganglion in anesthetized guinea pigs.
Did not induce hypothermia in conscious guinea pigs.
Did not cause bronchospasm in conscious guinea pigs.

Animal Model:

Cynomolgus monkey (conscious)^[2]
Dosage:

1 mg/kg; 3 mg/kg
Administration:

s.c.; single dose
Result:

Had no effect on cardiovascular parameters at 1 mg/kg s.c.
Produced modest, transitory cardiovascular effects with no morphological ECG alterations at 3 mg/kg s.c.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 181183-52-8
Appearance Solid
Molecular Weight 469.55
Formel C₂₁H₃₁N₃O₇S
Color White to off-white
SMILES

O=C(O)C(O)CC(O)=O.O=S(CC1=CC2=C(NC=C2CCN(C)C)C=C1)(N3CCCC3)=O
Synonyms

PNU180638
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (212.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 33.33 mg/mL (70.98 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1297 mL

10.6485 mL

21.2970 mL

5 mM

0.4259 mL

2.1297 mL

4.2594 mL

10 mM

0.2130 mL

1.0648 mL

2.1297 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (5.32 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.32 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.32 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.

Working Solution

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: 50 mg/mL (106.48 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Working solution concentration: 0.22 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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pascual J, et al. Almotriptan: a review of 20 years' clinical experience. Expert Rev Neurother. 2019;19(8):759-768. [Content Brief]

[2]. Gras J, et al. Almotriptan, a new anti-migraine agent: a review. CNS Drug Rev. 2002;8(3):217-234. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.1297 mL	10.6485 mL	21.2970 mL	53.2425 mL
	5 mM	0.4259 mL	2.1297 mL	4.2594 mL	10.6485 mL
	10 mM	0.2130 mL	1.0648 mL	2.1297 mL	5.3242 mL
	15 mM	0.1420 mL	0.7099 mL	1.4198 mL	3.5495 mL
	20 mM	0.1065 mL	0.5324 mL	1.0648 mL	2.6621 mL
	25 mM	0.0852 mL	0.4259 mL	0.8519 mL	2.1297 mL
	30 mM	0.0710 mL	0.3549 mL	0.7099 mL	1.7747 mL
	40 mM	0.0532 mL	0.2662 mL	0.5324 mL	1.3311 mL
	50 mM	0.0426 mL	0.2130 mL	0.4259 mL	1.0648 mL
	60 mM	0.0355 mL	0.1775 mL	0.3549 mL	0.8874 mL
DMSO	80 mM	0.0266 mL	0.1331 mL	0.2662 mL	0.6655 mL
DMSO	100 mM	0.0213 mL	0.1065 mL	0.2130 mL	0.5324 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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Almotriptan malate

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FDA Approved & Pharmacopeial Drug Library

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Antidepressant Compound Library

5-HT Receptor Compound Library

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MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Almotriptan malate

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Anti-Obesity Compound Library

Antidepressant Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Almotriptan malate Related Classifications

HY-B0383 Related Classifications