2. Metabolic Enzyme/Protease
  3. PANK
  4. Claziprotamidum

Claziprotamidum  (Synonyms: Claziprotamide; BBP-671)

Cat. No.: HY-159509
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Claziprotamidum (Claziprotamide; BBP-671) is a panthothenate kinase (PANK) activator with oral activity and blood-brain barrier permeability. Claziprotamidum binds to and activates all PANK isoforms, with the highest affinity for PANK3 (KD = 97 pM; IC50 = 1.39 nM). Claziprotamidum increases the intracellular biosynthesis of Coenzyme A (HY-128851) and restores mitochondrial function. Claziprotamidum can be used in the research of pantothenate kinase-associated neurodegeneration and propionic acidemia.

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

Claziprotamidum

Claziprotamidum Chemical Structure

CAS No. : 2361124-03-8

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Based on 1 publication(s) in Google Scholar

Claziprotamidum Related Antibodies

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PanK1 PanK2 PanK3

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Description

Claziprotamidum (Claziprotamide; BBP-671) is a panthothenate kinase (PANK) activator with oral activity and blood-brain barrier permeability. Claziprotamidum binds to and activates all PANK isoforms, with the highest affinity for PANK3 (KD = 97 pM; IC50 = 1.39 nM). Claziprotamidum increases the intracellular biosynthesis of Coenzyme A (HY-128851) and restores mitochondrial function. Claziprotamidum can be used in the research of pantothenate kinase-associated neurodegeneration and propionic acidemia[1][2][3].

IC50 & Target[3]

PanK3

1.39 nM (Ki)

PanK1β

2.02 nM (Ki)

PanK2

102 nM (Ki)

In Vitro

Claziprotamidum (10 μM; 24 h) increases total CoA levels by 244% in C3A human hepatocyte-like cells[1].
Claziprotamide (BBP-671) acts as an allosteric activator of recombinant PANK1β, PANK2, and PANK3 proteins by reducing their sensitivity to feedback inhibition by acetyl-CoA[2].
Claziprotamidum potently modulates the activity of recombinant human PANK1β, PANK2, and PANK3 proteins, with Ki values of 102 ± 21.4 nM, 2.02 ± 0.52 nM, and 1.39 ± 0.33 nM, respectively[3].
Claziprotamidum binds tightly to recombinant human PANK3 protein with a K0 of 97 ± 2 pM and a residence time of 21.4 minutes[3].
Claziprotamidum (2-7.5 μM) renders recombinant human PANK1β, PANK2, or PANK3 proteins, respectively, highly resistant to inhibition by propionyl-CoA[3].
Claziprotamidum (0.1-90 μM; 24 h) increases total intracellular CoA levels in human liver-derived C3A cells, with maximum elevation at 10 μM[3].

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

Claziprotamidum Related Antibodies
Parmacokinetics
Species Dose Route Tmax Cmax AUC0-inf Bioavailability C0 T1/2 CL Vss
Mice[1] 2 mg/kg i.v. / / 2151 ng·h/mL / 1968 ng/mL 0.7 h 15.5 0.89 L/kg
Mice[1] 10 mg/kg p.o. 0.25 h 3304 ng/mL 10022 ng·h/mL 93.2 % / / / /
In Vivo

Claziprotamidum (10 mg/kg; administered via oral gavage; once every 12 hours; 5 doses total) significantly and potently increases CoA concentrations in the liver, forebrain and hindbrain of mice compared with the vehicle control group, and its efficacy is comparable to that of the reference compound 2[1].
Claziprotamidum (0.1-10 mg/kg; p.o.; single administration) dose-dependently increases total CoA levels in the liver and forebrain of healthy C57BL/6J mice. At a single dose of 10 mg/kg, hepatic CoA levels increase by approximately 110%, and forebrain CoA levels increase by approximately 60%[2].
Claziprotamidum (0.1-30 mg/kg; p.o.; once daily; for 7 consecutive days) dose-dependently increases the drug concentrations in plasma, liver and forebrain of healthy C57BL/6J mice[2].
Claziprotamidum (10 mg/kg; p.o.; once daily; for 5 consecutive days) can cross the blood-brain barrier, increase the total CoA level in brain tissue, and also elevate the total CoA level in liver in healthy Sprague-Dawley rats treated with intracisternal catheterization[2].
Claziprotamidum (1 mg/kg; p.o.; once daily; for 3 consecutive days) transiently increases whole-blood acetyl-CoA levels in healthy C57BL/6J mice, with a peak reached at 4 h after the final administration[2].
Claziprotamidum (3 mg/kg/day; oral administration; via feed; once daily; for 5 consecutive days) doubles the whole-blood acetyl-CoA levels in healthy C57BL/6J mice[2].
Claziprotamidum (10 mg/kg per day; mixed into feed; ad libitum access; for 30 consecutive days) restores total brain CoA levels, increases body weight and improves motor function in Pank1fl/fl,Pank2fl/fl SynCre+ PKAN mice, but produces no statistically significant improvement in their survival rate[2].
Claziprotamidum (22.5 ppm; oral administration; continuous dosing) restores the survival rate of PA mice to 100%, normalizes hepatic CoA metabolite levels, reduces the levels of hallmark PA biomarkers in plasma and urine, and restores mitochondrial TCA cycle function[3].
Claziprotamidum (1 mg/kg; p.o.; single administration) increases the total hepatic CoA concentration in healthy C57BL/6J mice, with the peak observed at 4 h, and the elevated level persists for up to 24 h[3].
Claziprotamidum (11.25-45 ppm; oral administration; continuous dosing; 4 weeks) produces the maximal increase in total hepatic CoA concentration in healthy C57BL/6J mice at the dose of 22.5 ppm, with no additional benefit observed at the higher dose of 45 ppm[3].
Claziprotamidum (22.5 ppm; oral administration; continuous dosing) restores the survival rate of PA mice to 100%, normalizes hepatic CoA metabolite levels, reduces the levels of hallmark PA biomarkers in plasma and urine, and restores mitochondrial TCA cycle function[3].

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

Animal Model: C57Bl6/J (6−8 weeks old)[1]
Dosage: 10 mg/kg
Administration: oral gavage; every 12 hours; 5 doses
Result: Significantly increased total CoA levels in mouse liver, forebrain, and hindbrain relative to vehicle control.
Animal Model: C57BL/6J (male, 8-9 weeks old)[2]
Dosage: 0.1 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Left liver total CoA levels unchanged relative to controls at 0.1 mg/kg.
Increased liver total CoA to ~160 pmol/mg wet weight (a ~50% increase relative to controls) and forebrain total CoA to ~70 pmol/mg wet weight (a ~30% increase relative to controls) at 1 mg/kg.
Increased liver total CoA to ~190 pmol/mg wet weight (a ~80% increase relative to controls) and forebrain total CoA to ~78 pmol/mg wet weight (a ~45% increase relative to controls) at 3 mg/kg.
Increased liver total CoA to ~220 pmol/mg wet weight (a ~110% increase relative to controls) and forebrain total CoA to ~85 pmol/mg wet weight (a ~60% increase relative to controls) at 10 mg/kg.
Animal Model: C57BL/6J (male, 8 weeks old)[2]
Dosage: 0.1 mg/kg; 1 mg/kg; 3 mg/kg; 30 mg/kg
Administration: p.o.; once daily; 7 days
Result: Increased plasma, liver, and forebrain concentrations proportionally to the administered dose.
Animal Model: Sprague-Dawley (male, intracisternal cannulated)[2]
Dosage: 10 mg/kg
Administration: p.o.; once daily; 5 days
Result: Reached a Cmax of 0.12 pmol/μL and half-life of 1.6 hours in CSF.
Increased liver total CoA from a baseline of ~100 pmol/mg wet weight to a Cmax of ~142 pmol/mg wet weight at 2 hours postdose, with levels remaining elevated at 8 hours.
Increased brain total CoA from a baseline of ~40 pmol/mg wet weight to a Cmax of ~78 pmol/mg wet weight at 8 hours postdose.
Animal Model: C57BL/6J (male, 8-9 weeks old)[2]
Dosage: 1 mg/kg
Administration: p.o.; once daily; 3 days
Result: Increased whole-blood acetyl-CoA levels from a baseline of ~0.3 pmol/μL blood to a peak of ~0.55 pmol/μL blood at 4 hours postdose, then decreased to ~0.3 pmol/μL blood at 8 hours postdose.
Animal Model: C57BL/6J (8-10 weeks old)[2]
Dosage: 3 mg/kg/day
Administration: p.o.; via chow; once daily; 5 days
Result: Increased whole-blood acetyl-CoA levels by ~100% relative to untreated controls (from ~0.3 pmol/μL blood to ~0.6 pmol/μL blood).
Animal Model: Pank1fl/fl,Pank2fl/fl SynCre+ (mixed gender, postnatal day 14 at study start, neuron-specific conditional deletion of Pank1 and Pank2 genes via SynCre promoter)[2]
Dosage: 10 mg/kg/day
Administration: p.o.; via 75 ppm chow; ad libitum; 30 days starting at P14
Result: Was detected in plasma, liver, forebrain, and hindbrain of treated mice.
Elevated forebrain total CoA levels, restoring ~70% of the deficit relative to untreated PKAN mice, and fully restored hindbrain total CoA levels to control levels.
Increased body weight significantly relative to untreated PKAN mice.
Enhanced locomotor function, with total distance traveled increased by ~300% and percentage of time moving increased by ~200% relative to untreated PKAN mice.
Showed no statistically significant improvement in survival probability relative to untreated PKAN mice.
Animal Model: C57BL/6J mice (male and female, age postnatal day 19-21, genetic hypomorphic Propionic acidemia model with genotype Pcca^(-/-) PCCA(A138T)^(tg/0))[3]
Dosage: 22.5 ppm
Administration: oral; continuous
Result: Normalized hepatic nonesterified CoA (CoASH) and acetyl-CoA (C2-CoA) concentrations to near wild-type levels.
Reduced hepatic propionyl-CoA (C3-CoA) levels and significantly lowered the hepatic C3:C2-CoA ratio.
Significantly reduced elevated plasma C3:C2-carnitine ratio, methylcitrate, and methylmalonate.
Significantly reduced urinary malate, α-ketoglutarate, and C3:C2-carnitine ratio, while elevated urinary C2-carnitine.
Restored survival to wild-type levels, with 100% survival up to postnatal day 100.
Animal Model: C57BL/6J mice (male, age 8 weeks)[3]
Dosage: 1 mg/kg
Administration: p.o.; single dose
Result: Increased liver total CoA concentrations to a maximum at 4 hours post-dosing.
Remained elevated through 12 hours post-dosing.
Were still higher than baseline at 24 hours post-dosing.
Animal Model: C57BL/6J mice (male, age 8 weeks)[3]
Dosage: 11.25 ppm; 22.5 ppm; 45 ppm
Administration: oral; continuous; 4 weeks
Result: Elevated liver total CoA concentrations compared to control at 11.25 ppm.
Maximally elevated liver total CoA concentrations at 22.5 ppm.
Did not further increase liver total CoA concentrations at 45 ppm despite higher liver drug levels.
Molecular Weight

374.84

Formula

C19H20ClFN4O
CAS No.
Appearance

Solid

SMILES

O=C(CC1=CC=C(C2CC2)C(F)=C1)N3CCN(CC3)C4=NN=C(C=C4)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (266.78 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 2.6678 mL 13.3390 mL 26.6780 mL
5 mM 0.5336 mL 2.6678 mL 5.3356 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.

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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 (13.34 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    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% Corn Oil

    Solubility: ≥ 5 mg/mL (13.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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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:
%
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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.
Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6678 mL 13.3390 mL 26.6780 mL 66.6951 mL
5 mM 0.5336 mL 2.6678 mL 5.3356 mL 13.3390 mL
10 mM 0.2668 mL 1.3339 mL 2.6678 mL 6.6695 mL
15 mM 0.1779 mL 0.8893 mL 1.7785 mL 4.4463 mL
20 mM 0.1334 mL 0.6670 mL 1.3339 mL 3.3348 mL
25 mM 0.1067 mL 0.5336 mL 1.0671 mL 2.6678 mL
30 mM 0.0889 mL 0.4446 mL 0.8893 mL 2.2232 mL
40 mM 0.0667 mL 0.3335 mL 0.6670 mL 1.6674 mL
50 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3339 mL
60 mM 0.0445 mL 0.2223 mL 0.4446 mL 1.1116 mL
80 mM 0.0333 mL 0.1667 mL 0.3335 mL 0.8337 mL
100 mM 0.0267 mL 0.1334 mL 0.2668 mL 0.6670 mL
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Claziprotamidum Related Classifications

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    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.

Keywords:

Claziprotamidum2361124-03-8Claziprotamide BBP-671BBP671BBP 671BBP-671PANKPantothenate Kinasepantothenate kinase (PANK)PANK2PANK3coenzyme Apantothenate kinase-associated neurodegenerationPANK1a/bC3A human hepatocyte-like cellsacyl-CoAsacetyl-CoAPANK-deficient mouse modelsInhibitorinhibitorinhibit

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