WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H528001
CAS#: 1380341-99-0
Description: GAL-021 is a large conductance calcium-activated potassium channel (BKCa-channel) blocker potentially for the treatment of respiratory depression. GAL-021 inhibited KCa1.1 in GH3 cells, and the evoked ventilatory stimulation was attenuated in Slo1 mice lacking the pore-forming α-subunit of the KCa1.1 channel. At a higher concentration of GAL-160 (100 μM), inhibition of the delayed rectifier K(+) current and leak K(+) current were observed.
Hodoodo Cat#: H528001
Name: GAL-021
CAS#: 1380341-99-0
Chemical Formula: C11H22N6O
Exact Mass: 254.19
Molecular Weight: 254.338
Elemental Analysis: C, 51.95; H, 8.72; N, 33.04; O, 6.29
Synonym: GAL-021; GAL 021; GAL021
IUPAC/Chemical Name: 6-(methoxy(methyl)amino)-N2,N4-dipropyl-1,3,5-triazine-2,4-diamine
InChi Key: FJNLCHNQVJVCPY-UHFFFAOYSA-N
InChi Code: InChI=1S/C11H22N6O/c1-5-7-12-9-14-10(13-8-6-2)16-11(15-9)17(3)18-4/h5-8H2,1-4H3,(H2,12,13,14,15,16)
SMILES Code: CCCNC1=NC(N(OC)C)=NC(NCCC)=N1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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The following data is based on the product molecular weight 254.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Golder FJ, Dax S, Baby SM, Gruber R, Hoshi T, Ideo C, Kennedy A, Peng S, Puskovic V, Ritchie D, Woodward R, Wardle RL, Van Scott MR, Mannion JC, MacIntyre DE. Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator. Anesthesiology. 2015 Nov;123(5):1093-104. doi: 10.1097/ALN.0000000000000844. PubMed PMID: 26352381.
2: Dallas ML, Peers C, Golder FJ, Baby S, Gruber R, MacIntyre DE. GAL-021 and GAL-160 are Efficacious in Rat Models of Obstructive and Central Sleep Apnea and Inhibit BKCa in Isolated Rat Carotid Body Glomus Cells. Adv Exp Med Biol. 2015;860:361-70. doi: 10.1007/978-3-319-18440-1_41. PubMed PMID: 26303501.
3: McLeod JF, Leempoels JM, Peng SX, Dax SL, Myers LJ, Golder FJ. GAL-021, a new intravenous BKCa-channel blocker, is well tolerated and stimulates ventilation in healthy volunteers. Br J Anaesth. 2014 Nov;113(5):875-83. doi: 10.1093/bja/aeu182. PubMed PMID: 24989775.
4: Roozekrans M, Olofsen E, van der Schrier R, van Gerven J, Peng S, McLeod J, Dahan A. Reversal of opioid-induced respiratory depression by BK-channel blocker GAL021: A pharmacokinetic-pharmacodynamic modeling study in healthy volunteers. Clin Pharmacol Ther. 2015 Jun;97(6):641-9. doi: 10.1002/cpt.99. PubMed PMID: 25704491.
5: Roozekrans M, van der Schrier R, Okkerse P, Hay J, McLeod JF, Dahan A. Two studies on reversal of opioid-induced respiratory depression by BK-channel blocker GAL021 in human volunteers. Anesthesiology. 2014 Sep;121(3):459-68. doi: 10.1097/ALN.0000000000000367. PubMed PMID: 25222672.
6: van der Schier R, Roozekrans M, van Velzen M, Dahan A, Niesters M. Opioid-induced respiratory depression: reversal by non-opioid drugs. F1000Prime Rep. 2014 Sep 4;6:79. doi: 10.12703/P6-79. Review. PubMed PMID: 25343036; PubMed Central PMCID: PMC4173639.
7: Golder FJ, Hewitt MM, McLeod JF. Respiratory stimulant drugs in the post-operative setting. Respir Physiol Neurobiol. 2013 Nov 1;189(2):395-402. doi: 10.1016/j.resp.2013.06.010. Review. PubMed PMID: 23791825.
8: Cotten JF. The latest pharmacologic ventilator. Anesthesiology. 2014 Sep;121(3):442-4. doi: 10.1097/ALN.0000000000000368. PubMed PMID: 25222671; PubMed Central PMCID: PMC4166568.
9: Xie Y, Puscheck EE, Rappolee DA. Effects of SAPK/JNK inhibitors on preimplantation mouse embryo development are influenced greatly by the amount of stress induced by the media. Mol Hum Reprod. 2006 Apr;12(4):217-24. PubMed PMID: 16574700.
