2. Neuronal Signaling
  3. Glucosylceramide Synthase (GCS)
  4. CCG-203586

CCG-203586 is a brain-penetrant glucosylceramide synthase (GCS) inhibitor. CCG-203586 reduces GCS production and brain levels, blocks the first committed step in ganglioside biosynthesis, and lowers downstream ganglioside levels. CCG-203586 can be used for the research of Tay-Sachs, Sandhoff disease, and types 2 and 3 Gaucher disease.

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

CCG-203586

CCG-203586 Chemical Structure

CAS No. : 1430611-23-6

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

CCG-203586 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CCG-203586 is a brain-penetrant glucosylceramide synthase (GCS) inhibitor. CCG-203586 reduces GCS production and brain levels, blocks the first committed step in ganglioside biosynthesis, and lowers downstream ganglioside levels. CCG-203586 can be used for the research of Tay-Sachs, Sandhoff disease, and types 2 and 3 Gaucher disease[1][2][3].

In Vitro

CCG-203586 (Compound 2) (1 h) inhibits glucosylceramide synthase activity in MDCK cell homogenates with an IC50 of 27 nM[1].
CCG-203586 (24 h) reduces glucosylceramide levels in intact MDCK cells with an IC50 of 15.3 nM[1].
CCG-203586 (1 μM) has a half-life of 2.5 min when incubated with CD-1 mouse liver microsomes[1].
CCG-203586 (1 μM) has a half-life of 28 min when incubated with human liver microsomes[1].
CCG-203586 (Compound 3h) (24 h) inhibits glucosylceramide production in MDR1-MDCKII cells with an IC50 of 24.3 nM[2].

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

CCG-203586 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-∞ (Brain) AUC0-∞ (Plasma)
Mice[1] 10 mg/kg i.p. 36 h·ng/g 317 ng·h/mL
In Vivo

CCG-203586 (Compound 2) (60 mg/kg; i.p.; daily; 3 days) reduces brain GCS levels in normal C57BL/6 mice by 17%[1].
CCG-203586 (Compound 3h) (10-60 mg/kg/day; i.p.; 3 days) produces a dose-dependent reduction in brain glucosylceramide levels in healthy C57BL/6 mice, with concurrent significant reductions in kidney and liver glucosylceramide at the higher dose[2].
CCG-203586 (60 mg/kg; i.p.; daily; 7 days) administered to juvenile Sandhoff mice significantly reduces ganglioside (GM2, total sialic acid) and GA2 storage in brain and liver, with a 41% reduction in liver glucosylceramide, while showing no adverse effects on brain development or body weight[3].

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

Animal Model: C57BL/6 (6−8 weeks old, mixed gender)[1]
Dosage: 60 mg/kg
Administration: i.p.; daily; 3 days
Result: Induced a 17% reduction in brain glucosylceramide levels relative to vehicle control.
Animal Model: C57BL/6 (6- to 8-week-old, female or male)[2]
Dosage: 10 mg/kg/day; 60 mg/kg/day
Administration: i.p.; daily; 3 days
Result: Reduced brain GlcCer levels by 10% at 10 mg/kg/day compared to vehicle controls.
Reduced kidney GlcCer levels significantly at 10 mg/kg/day compared to vehicle controls.
Caused no significant change in liver GlcCer levels at 10 mg/kg/day compared to vehicle controls.
Reduced brain GlcCer levels by 17% at 60 mg/kg/day compared to vehicle controls.
Reduced liver and kidney GlcCer levels significantly at 60 mg/kg/day compared to vehicle controls.
Was well tolerated at both doses with no observed weight loss or adverse behavioral, gastrointestinal, or respiratory changes.
Animal Model: SV/129 Hexb-/- (Sandhoff) (juvenile, postnatal day 9 to 15, Sandhoff disease model via Hexb gene disruption via homologous recombination and embryonic stem cell technology)[3]
Dosage: 60 mg/kg
Administration: i.p.; daily; 7 days
Result: Reduced total ganglioside sialic acid by 11% in cerebrum (to 432 μg/100 mg dry weight), 14% in cerebellum (to 318 μg/100 mg dry weight), and 38% in liver (to 70 μg/100 mg dry weight) relative to PBS-treated controls.
Reduced GM2 content by 52% in cerebrum (to 12.3 μg sialic acid/100 mg dry weight) and 53% in cerebellum (to 9.8 μg sialic acid/100 mg dry weight); reduced liver NGNA-GM2 by 45% (to 42.1 μg sialic acid/100 mg dry weight).
Reduced GA2 content significantly in cerebrum (to 0.51 mg/100 mg dry weight) and cerebellum (to 0.55 mg/100 mg dry weight) relative to controls.
Reduced liver glucosylceramide (GlcCer) by an average of 41% (to an average of 3.27 μg/100 mg dry weight) relative to controls.
Showed no significant difference in brain weight, brain water content, β-hexosaminidase specific activity, β-galactosidase specific activity, and cholesterol/neutral/acidic phospholipid distribution from PBS-treated controls.
Resulted in slightly higher body weight of treated mice (9.0 g) compared to PBS-treated Hexb-/- controls (7.8 g) and comparable to normal Hexb+/- mice.
Molecular Weight

436.55

Formula

C26H32N2O4
CAS No.
Appearance

Solid

SMILES

[C@@H]([C@@H](CN1CCCC1)NC(CC2CC=3C(C2)=CC=CC3)=O)(O)C=4C=C5C(=CC4)OCCO5
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)

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CCG-203586 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

CCG-2035861430611-23-6CCG203586CCG 203586Glucosylceramide Synthase (GCS)lysosomal storage diseasesglucosylceramide synthaseganglioside biosynthesishuman liver microsomesSandhoff miceC57BL/6 miceblood-brain barrierMDCK cellsCD-1 mouse liver microsomesP-glycoproteinInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CCG-203586
Cat. No.:
HY-206259
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.