Art. -Nr.: HY-12848C

SAG dihydrochloride

Name: SAG dihydrochloride
Brand: MedChemExpress
SKU: HY-12848C
Price: 60.00 USD
Availability: InStock
Rating: 5 (46 reviews)

46 Cited Publications

Kundenbewertung

Based on 46 publication(s) in Google Scholar

SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC₅₀=3 nM; K_d=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.

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Reinheit : 98.23%
CAS. Nr.: 2702366-44-5
Formel: C₂₈H₃₀Cl₃N₃OS
Molecular Weight:562.98

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

SAG dihydrochloride Chemical Structure

CAS. Nr.: 2702366-44-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (46)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 3 nM (Smo)^[1]

In Vitro

SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC₅₀ of 3 nM and then inhibits expression at higher concentrations^[1].
SAG (1-1000 nM; 1 h) competes for the binding of BODIPY-cyclopamine to Smo-expressing Cos-1 cells, yielding an apparent dissociation constant (K_d) of 59 nM for the SAG/Smo complex^[1].
SAG (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin^[2].
SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells^[3].
SAG (250 nM; 24 and 48 h) increases CAXII mRNA expression in MDAMB231 cells at 24h in normoxic and hypoxic conditions in MDAMB231 cells^[3].
SAG (250 nM; 24 h) increases MDAMB231 cells migration^[3].

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

In Vivo

SAG (1.0 mM) induces more osteogenesis mainly at the defect borders and a significant increase in BV/TV at the eight week timepoint in CD-1 mice^[4].
SAG (15-20 mg/kg; i.p.) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice^[5].

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

Animal Model:

Pregnant C57BL/6J mice^[5]
Dosage:

15, 17, 20 mg/kg
Administration:

A single i.p.
Result:

Effective in ca. 80% of the embryos and increased Gli1 and Gli2 mRNA expression in the limb bud, with Gli1 mRNA being the most upregulated at the dose of 20 mg/kg.

Chemical Information

CAS. Nr. 2702366-44-5
Appearance Solid
Molecular Weight 562.98
Formel C₂₈H₃₀Cl₃N₃OS
Color Light yellow to light brown
SMILES

O=C(C1=C(Cl)C2=CC=CC=C2S1)N([C@H]3CC[C@H](NC)CC3)CC4=CC=CC(C5=CC=NC=C5)=C4.[H]Cl.[H]Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (46)

All RT-PCRIFCell Migration/Invasion AssayFlow CytometryWB

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Journal Impact Factor

Cell Res

Cholesterylation of Smoothened is a calcium-accelerated autoreaction involving an intramolecular ester intermediate. [Abstract]

2022 Mar;32(3):288-301. PMID: 35121857

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Mar;32(3):288-301. [Abstract]

SAG (5-200 nM)-induced Gli1 expression is independent of extracellular Ca²⁺ concentration. Sub-confluent NIH3T3 cells were serum-starved in 0.5% FCS overnight and switched to normal DMEM or Ca²⁺-free DMEM containing indicated concentration of SAG. Cells were harvested for RNA extraction after 6 hours.
Cell Stem Cell

Establishing dorsal-ventral patterning in human neural tube organoids with synthetic organizers. [Abstract]

2025 Jul 3;32(7):1071-1086.e8. PMID: 40373768
Nat Commun

Identification of a component of the tubulin poly-glutamylase complex required for phosphoinositide homeostasis and cilium assembly and maintenance. [Abstract]

2026 May 15. PMID: 42140944
Nat Commun

Phosphorylation of human glioma-associated oncogene 1 on Ser937 regulates Sonic Hedgehog signaling in medulloblastoma. [Abstract]

2024 Feb 2;15(1):987. PMID: 38307877
Adv Sci (Weinh)

Primary Cilia Formation Mediated by Hsa_Circ_0005185/OTUB1/RAB8A Complex Inhibits Prostate Cancer Progression by Suppressing Hedgehog Signaling Pathway. [Abstract]

2025 Feb;12(8):e2411675. PMID: 39785769
Sci Adv

Noncanonical UPR factor CREB3L2 drives immune evasion of triple-negative breast cancer through Hedgehog pathway modulation in T cells. [Abstract]

2025 Jan 10;11(2):eads5434. PMID: 39792663

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jan 10;11(2):eads5434. [Abstract]

SAG hydrochloride (500 nM) increased the RNA expression of Ptch1 and Gli1 in active CD8⁺ T cells and active CD8⁺ T cells cocultured with D2A1 cells.

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jan 10;11(2):eads5434. [Abstract]

SAG hydrochloride (500 nM) decreased the percentage of the CD25⁺CD8⁺ population in active CD8⁺ T cells.

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jan 10;11(2):eads5434. [Abstract]

SAG hydrochloride (500 nM) decreased the gene expression of Gzmb and IFN-γ in active CD8⁺ T cells cocultured with D2A1 cells.
Sci Adv

Yap controls notochord formation and neural tube patterning by integrating mechanotransduction with FoxA2 and Shh expression. [Abstract]

2023 Jun 16;9(24):eadf6927. PMID: 37315133

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 16;9(24):eadf6927. [Abstract]

Representative immunofluorescent images of TdTomato (tdTom) and brachyury (T) at E10.5 in trunk cross sections of indicated genotypes with or without small molecule agonist (SAG, 20 mg/kg; i.p.) treatment. Scale bar, 100 μm.
Cell Commun Signal

TGFβ1-induced hedgehog signaling suppresses the immune response of brain microvascular endothelial cells elicited by meningitic Escherichia coli. [Abstract]

2024 Feb 15;22(1):123. PMID: 38360663

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Feb 15;22(1):123. [Abstract]

qPCR detecting expression alterations of IL-6, MIP-2, and E-selectin in RS218 infected hBMECs with or without SAG pre-treatment (at 10 μM).

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Feb 15;22(1):123. [Abstract]

Western blot detecting expression of E-selectin, KRAS and ERK1/2 phosphorylation in RS218 infected hBMECs with or without SAG pre-treatment (at 10 μM).

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Feb 15;22(1):123. [Abstract]

IF assays showing the E-selectin and KRAS expression in brains of mice challenged by RS218 with or without SAG (10 mg/kg, i.v.; single dose) pre-treatment. The E-selection and KRAS were stained in red. CD31 was specifically applied for labeling the micro-vessels in green. The cell nucleus was stained in blue with DAPI. Scale bar = 50 μm
Cell Mol Gastroenterol Hepatol

Triggering Receptor Expressed on Myeloid Cells 2+ Macrophages Promote Pancreatic Regeneration Through Cholesterol-Metabolism Reprogramming and Hedgehog Signaling Activation Following Acute Pancreatitis. [Abstract]

2026 May 27:101819. PMID: 42208763
Cell Rep

2020 Apr.
Neurosci Bull

2026 Jul 6. PMID: 42406285
Biomater Adv

A supramolecular MgTA@MnO₂ nanozyme platform supports human spinal cord organoid structural integration and locomotor recovery via microenvironmental reprogramming. [Abstract]

2026 Jun 16:188:215018. PMID: 42309040
Ecotoxicol Environ Saf

Zearalenone at environmental levels promoted ER- positive breast cancer cell lines through the hedgehog pathway. [Abstract]

2025 Sep 15:303:118813. PMID: 40773915
Biochem Pharmacol

Identification of pseudolaric acid B as a novel Hedgehog pathway inhibitor in medulloblastoma. [Abstract]

2021 Aug:190:114593. PMID: 33964282
Cell Rep Methods

Effective cryopreservation of human brain tissue and neural organoids. [Abstract]

2024 May 20;4(5):100777. PMID: 38744289
Int J Mol Sci

2026 Jul 22;27(14):6507. PMID: 42511848
Glia

RXR Gamma Enables Oligodendrocyte Differentiation by Suppressing Sonic Hedgehog Signaling. [Abstract]

2026 Jun;74(6):e70151. PMID: 41934103
Glia

Deubiquitinase USP18 regulates reactive astrogliosis by stabilizing SOX9. [Abstract]

2021 Jul;69(7):1782-1798. PMID: 33694203
J Pathol

Transcriptomic profiling reveals the role of Hedgehog signaling as a biomarker and in the pathogenesis of Ménétrier's disease. [Abstract]

2025 Nov 6. PMID: 41199529
Molecules

Synthesis and Smo Activity of Some Novel Benzamide Derivatives. [Abstract]

2017 Dec 31;23(1):85. PMID: 29301237
Sci Rep

Tanshinone IIA inhibits foam cell formation and alleviates atherosclerosis by regulating the Hedgehog signaling pathway through TRPM2 suppression. [Abstract]

2026 May 18. PMID: 42151241
Sci Rep

Ptbp1 knockdown induces conversion of rat spinal cord astrocytes into neuron like cells. [Abstract]

2025 Oct 14;15(1):35928. PMID: 41087401
Cancer Sci

Transcription factor POU4F2 promotes colorectal cancer cell migration and invasion through hedgehog-mediated epithelial-mesenchymal transition. [Abstract]

2021 Oct;112(10):4176-4186. PMID: 34327778

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2021 Oct;112(10):4176-4186. [Abstract]

SAG hydrochloride (SAG; 500 nM; 24, 48 h) rescued the migration, which was inhibited by the knockdown of POU4F2 in HCT116 cells.

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2021 Oct;112(10):4176-4186. [Abstract]

SAG hydrochloride (SAG; 500 nM; 24 h) increased the levels of SHH, PTCH1, SMO, and GLI‐1 in shPOU4F2‐transfected HCT116 cells.
J Cell Mol Med

Whole-exome sequencing identified novel variants in CPLANE1 that causes oral-facial-digital syndrome Ⅵ by inducing primary cilia abnormality. [Abstract]

2022 Jun;26(11):3213-3222. PMID: 35582950
iScience

Modeling the precise interaction of glioblastoma with human brain region-specific organoids. [Abstract]

2024 Feb 5;27(3):109111. PMID: 38390494
iScience

Generation of dorsoventral human spinal cord organoids via functionalizing composite scaffold for drug testing. [Abstract]

2022 Dec 26;26(1):105898. PMID: 36647382
Biomedicines

Generation of a Pure Culture of Neuron-like Cells with a Glutamatergic Phenotype from Mouse Astrocytes. [Abstract]

2022 Apr 18;10(4):928. PMID: 35453678
Drug Dev Res

Curcumin mitigates the epithelial-to-mesenchymal transition in biliary epithelial cells through upregulating CD109 expression. [Abstract]

2019 Nov;80(7):992-999. PMID: 31403228
Toxins

Human-Relevant Sensitivity of iPSC-Derived Human Motor Neurons to BoNT/A1 and B1. [Abstract]

2021 Aug 22;13(8):585. PMID: 34437455
Development

Enpp1 inhibits ectopic joint calcification and maintains articular chondrocytes by repressing hedgehog signaling. [Abstract]

2018 Sep 20;145(18):dev164830. PMID: 30111653

SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Development. 2018 Sep 20;145(18):dev164830. [Abstract]

WT MEF cells are treated with 100 nM SAG, 0.1mM ATP, or 0.1mM NHATP for 10 min (U). p-Creb, total Creb and Tubulin protein levels are detected by Western blotting.
J Tradit Complement Med

2025 Jun 14.
J Biomed Mater Res A

GelMA Hydrogel Encapsulating iPSC-Derived Human Spinal Cord Organoids Enhances Neural Regeneration and Restores Motor Function in Rat Spinal Cord Injury. [Abstract]

2025 Oct;113(10):e38001. PMID: 41051068
Mol Brain

Meningitic Escherichia coli α-hemolysin aggravates blood-brain barrier disruption via targeting TGFβ1-triggered hedgehog signaling. [Abstract]

2021 Jul 19;14(1):116. PMID: 34281571
J Pharm Biomed Anal

Rapid discovery of cyclopamine analogs from Fritillaria and Veratrum plants using LC-Q-TOF-MS and LC-QqQ-MS. [Abstract]

2017 Aug 5:142:201-209. PMID: 28521273
Neuroscience

Trichostatin A-primed spinal cord organoids alleviate oxidative stress and improve recovery after spinal cord injury involving the NRF2/HO-1 signaling pathway. [Abstract]

2026 Jun 6:610:122-135. PMID: 42250855
Exp Eye Res

The effects of pigment epithelium-derived factor and associated peptides on the differentiation of retinal ganglion cells from human-induced pluripotent stem cells. [Abstract]

2025 Aug:257:110440. PMID: 40409357
Tissue Cell

The Shh-p38-NFATc1 signaling pathway is essential for osteoclastogenesis during tooth eruption. [Abstract]

2025 Feb:92:102643. PMID: 39612595
bioRxiv

Rapid Remodeling of Human White Adipose Tissue Following Bariatric Surgery. [Abstract]

2026 Apr 15:2026.04.09.717542. PMID: 42039637
Res Sq

2026 Feb 2.
bioRxiv

Neuronal Cell-Cycle Re-entry Defines Divergent Outcomes Through Replication-Dependent DNA Damage in ALS. [Abstract]

2026 Feb 16:2026.02.13.705790. PMID: 41756973
bioRxiv

2025 July 21.
bioRxiv

2025 March 25.
Patent

US20240247230A1.
UNIVERSIDAD DE CONCEPCIÓN

2023 Apr.
Research Square Preprint

2021 Sep.
University of Bonn

2021 May 21.

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 100 mg/mL (177.63 mM; Need ultrasonic)

DMSO : 33.33 mg/mL (59.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7763 mL

8.8813 mL

17.7626 mL

5 mM

0.3553 mL

1.7763 mL

3.5525 mL

10 mM

0.1776 mL

0.8881 mL

1.7763 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 50 mg/mL (88.81 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen JK, et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6. [Content Brief]

[2]. Stanton BZ, et al. A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol. 2009 Mar;5(3):154-6. [Content Brief]

[3]. Guerrini G, et, al. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec; 233(12): 9799-9811. [Content Brief]

[4]. Lee S, et al. Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg. 2017 Feb 13. [Content Brief]

[5]. Fish EW, et al. Preaxial polydactyly following early gestational exposure to the smoothened agonist, SAG, in C57BL/6J mice. Birth Defects Res A Clin Mol Teratol. 2016 Nov 1. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	1.7763 mL	8.8813 mL	17.7626 mL	44.4066 mL
	5 mM	0.3553 mL	1.7763 mL	3.5525 mL	8.8813 mL
	10 mM	0.1776 mL	0.8881 mL	1.7763 mL	4.4407 mL
	15 mM	0.1184 mL	0.5921 mL	1.1842 mL	2.9604 mL
	20 mM	0.0888 mL	0.4441 mL	0.8881 mL	2.2203 mL
	25 mM	0.0711 mL	0.3553 mL	0.7105 mL	1.7763 mL
	30 mM	0.0592 mL	0.2960 mL	0.5921 mL	1.4802 mL
	40 mM	0.0444 mL	0.2220 mL	0.4441 mL	1.1102 mL
	50 mM	0.0355 mL	0.1776 mL	0.3553 mL	0.8881 mL
H₂O	60 mM	0.0296 mL	0.1480 mL	0.2960 mL	0.7401 mL
	80 mM	0.0222 mL	0.1110 mL	0.2220 mL	0.5551 mL
	100 mM	0.0178 mL	0.0888 mL	0.1776 mL	0.4441 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Bioz

Keywords

SAG dihydrochloride

46 Cited Publications

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SAG dihydrochloride

Publications Citing Use of MedChemExpress (MCE) SAG dihydrochloride