1. Metabolic Enzyme/Protease
  2. Endogenous Metabolite
  3. Sapropterin dihydrochloride

Sapropterin dihydrochloride  (Synonyms: (6R)-BH4 dihydrochloride; (6R)-Tetrahydro-L-biopterin dihydrochloride)

Art. -Nr.: HY-A0124A Reinheit: 99.61%
Handling Instructions Technical Support

Sapropterin ((6R)-BH4; (6R)-Tetrahydro-L-biopterin) dihydrochloride is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin dihydrochloride can be used in study of phenylketonuria (PKU) phenylketonuria. Sapropterin dihydrochloride can aggravate experimental autoimmune encephalomyelitis (EAE).

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Sapropterin dihydrochloride

Sapropterin dihydrochloride Chemische Struktur

CAS. Nr. : 69056-38-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Based on 2 publication(s) in Google Scholar

Other Forms of Sapropterin dihydrochloride:

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Beschreibung

Sapropterin ((6R)-BH4; (6R)-Tetrahydro-L-biopterin) dihydrochloride is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin dihydrochloride can be used in study of phenylketonuria (PKU) phenylketonuria. Sapropterin dihydrochloride can aggravate experimental autoimmune encephalomyelitis (EAE)[1][2].

In Vitro

Sapropterin dihydrochloride enhances residual phenylalanine hydroxylase activity to increase phenylalanine oxidation[1].

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

In Vivo

Sapropterin (100 mg/kg/day; oral; daily; 22 days) dihydrochloride treatment aggravates primary progressive and relapsing-remitting EAE in SJL/J mice, as evidenced by increased clinical EAE scores, elevated plasma long-chain ceramide levels, reduced linolenic acid levels, and increased spinal cord T-cell infiltration[2].

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

Animal Model: SJL/J (female, 10-12-week-old, primary progressive and PLP-induced-relapsing-remitting EAE)[2]
Dosage: 100 mg/kg/day
Administration: oral; daily; 22 days
Result: Reached higher maximum clinical EAE scores and showed a significant increase in the area under the curve (AUC) of EAE scores.
Elevated plasma levels of long-chain ceramides (C14Cer, C16Cer, C18Cer, C20Cer, C18GluCer, C24:1GluCer).
Reduced plasma linolenic acid (FA18:3) levels and increased plasma levels of the endocannabinoid 1+2AG.
Showed no significant effect on peripheral T-cell proliferation or subpopulations in the spleen, but increased infiltration of CD4+ and CD8+ T-cells in the spinal cord.
Klinische Studie
Molekulargewicht

314.17

Formel

C9H17Cl2N5O3

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N=C(N)NC2=C1N[C@@H]([C@@H](O)[C@@H](O)C)CN2.[H]Cl.[H]Cl

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, stored under nitrogen, away from moisture

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

Lösungsmittel & Löslichkeit
In Vitro: 

H2O : 100 mg/mL (318.30 mM; Need ultrasonic)

DMSO : 100 mg/mL (318.30 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 3.1830 mL 15.9150 mL 31.8299 mL
5 mM 0.6366 mL 3.1830 mL 6.3660 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 (stored under nitrogen, 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

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 5 mg/mL (15.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (15.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
Reinheit & Dokumentation

Purity: 99.82%

Verweise

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 (stored under nitrogen, 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 / DMSO 1 mM 3.1830 mL 15.9149 mL 31.8299 mL 79.5747 mL
5 mM 0.6366 mL 3.1830 mL 6.3660 mL 15.9149 mL
10 mM 0.3183 mL 1.5915 mL 3.1830 mL 7.9575 mL
15 mM 0.2122 mL 1.0610 mL 2.1220 mL 5.3050 mL
20 mM 0.1591 mL 0.7957 mL 1.5915 mL 3.9787 mL
25 mM 0.1273 mL 0.6366 mL 1.2732 mL 3.1830 mL
30 mM 0.1061 mL 0.5305 mL 1.0610 mL 2.6525 mL
40 mM 0.0796 mL 0.3979 mL 0.7957 mL 1.9894 mL
50 mM 0.0637 mL 0.3183 mL 0.6366 mL 1.5915 mL
60 mM 0.0530 mL 0.2652 mL 0.5305 mL 1.3262 mL
80 mM 0.0398 mL 0.1989 mL 0.3979 mL 0.9947 mL
100 mM 0.0318 mL 0.1591 mL 0.3183 mL 0.7957 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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Sapropterin dihydrochloride
Art. -Nr.:
HY-A0124A
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