LTGO-33 free base · Synonyms: LTGO 33 · LTGO33
LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor.
For research use only. Not for human or veterinary use.
LTGO-33 structure
CAS No.: 2834106-06-6
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 50 mg | USD 496.00 | BP-02262-50mg | In stock | Get quote |
| 100 mg | USD 650.00 | BP-02262-100mg | In stock | Get quote |
| 250 mg | USD 1,150.00 | BP-02262-250mg | In stock | Get quote |
| 500 mg | USD 1,885.00 | BP-02262-500mg | In stock | Get quote |
| 1 g | Inquire | BP-02262-1g | In stock | Inquire |
| 2 g | Inquire | BP-02262-2g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9.
Biological activity
In Vitro LTGO-33 exhibits an IC50 of 33 nM from the closed state and 24 nM from an inactivated state. LTGO-33 displays species specificity for primate NaV1.8 over dog and rodent NaV1.8 and inhibits action potential firing in human dorsal root ganglia neurons. LTGO-33 inhibits TTX-R currents in primary DRG neurons from human (male donors: IC50 of 110 nM, 95% CI: 92 to 120 nM, n = 3-15 neurons per concentration; female donors: IC50 of 120 nM, 95% CI: 100 to 140 nM, 4- 6 neurons per concentration) and cynomolgus monkey (IC50 of 100 nM, 95% CI: 71 to 150 nM, n = 6 cells) but is markedly less effective on DRG neurons from dog (IC50 >10 µM, n = 6 cells), rat (IC50 >30 µM, n = 7 cells), and mouse (IC50 >30 µM, n = 8 cells). LTGO-33 stabilizs the deactivated state of VSDII, effectively keeping the channel closed by preventing movement of VSDII.
Identifiers
- SMILES
-
C(NC1=CC(S(C)(=N)=O)=CC=C1)(=O)C2=C(OC3=C(C)C=C(F)C=C3)N=CC(C(F)(F)F)=C2 - InChIKey
-
IIJWTXGHWFZLBF-UHFFFAOYSA-N
Specifications
- MW (average)
- 467.4370
- Formula
- C21H17F4N3O3S
- CAS No.
- 2834106-06-6
- Physical state
- Solid
- Color
- Off-white to light yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO
- In vitro
- DMSO : 100 mg/mL