Home > Products > Featured products

GFB-8438

  Cat. No.:  DC28702   Featured
Chemical Structure
2304549-73-1
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2304549-73-1
Synonyms: GFB-8438;GFB 8438;GFB8438
SMILES: O=C1N(CC2C(C(F)(F)F)=CC=CC=2)CCN(C2C=NNC(=O)C=2Cl)C1
Formula: C16H14ClF3N4O2
M.Wt: 386.76
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Yu M, et al.Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model.ACS Med Chem Lett. 2019 Oct 22;10(11):1579-1585.
Description: GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model[1].
Target: hTRPC5:0.18 μM (IC50) hTRPC4:0.29 μM (IC50) rTRPC5:0.18 μM (IC50)
In Vivo: GFB-8438 (30 mg/kg; s.c.; daily for 3 weeks) is efficacious in a hypertensive deoxycorticosterone acetate (DOCA)-salt rat model of focal segmental glomerulosclerosis (FSGS), significantly reducing both total protein and albumin concentrations in urine[1]. GFB-8438 (1 mg/kg; i.v.) treatment shows the Cl, VSS, and t1/2 were 31 mL/min/kg, 1.17 L/kg, and 0.5 hours, respectively[1]. Animal Model: Sprague Dawley rats (DOCA-salt rat model of FSGS)[1] Dosage: 30 mg/kg Administration: s.c.; daily for 3 weeks Result: Significant reduction in urine protein concentrations. Animal Model: 6-8 weeks old male SD rats[1] Dosage: 1 mg/kg Administration: i.v. (Pharmacokinetic Analysis) Result: The Cl, Vss, and t1/2 were 31 mL/min/kg, 1.17 L/kg, and 0.5 hours, respectively.
In Vitro: Pretreatment of mouse podocyte with GFB-8438 (1 μM for 30 min), followed by incubation with protamine sulfate, effectively blocked synaptopodin loss and cytoskeletal remodeling[1].
References: [1]. Yu M, et al.Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model.ACS Med Chem Lett. 2019 Oct 22;10(11):1579-1585.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC47315 ML-SI3 ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively.
DC46872 Evifacotrep Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases.
DC46871 Vocacapsaicin Vocacapsaicin (CA-008), a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief.
DC46377 ML-SA1 ML-SA1, as a selective TRPML agonist, inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 value of ML-SA1 against DENV2 RNA and ZIKV RNA is 8.3 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral.
DC45287 TRPC6-PAM-C20 TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).
DC28758 Umbellulone Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.
DC28702 GFB-8438 GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
DC11325 RN-1734 RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4α-phorbol 12,13-didecanoate with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively.
DC11508 AC1903 AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia